Advances in MRSA drug discovery: Where are we and where do we need to be?

Expert Opinion on Drug Discovery

Volumn 8, Issue 9, 2013, Pages 1095-1116

  Kurosu, Michio ^a   Siricilla, Shajila ^a   Mitachi, Katsuhiko ^a  

^a UNIVERSITY OF TENNESSEE HEALTH SCIENCE CENTER   (United States)

Author keywords

lactamase inhibitor; Acyl t RNA synthase inhibitor; Antibacterial agents; Antibacterial vaccine; Antibiotics; Antimicrobial peptides; Clp protease inhibitor; Combination therapy; Daptomycin; Dihydrofolate reductase inhibitor; Dihydropteroate synthase inhibitor; Electron transport inhibitor; Elongation factor G inhibitor; FAS II inhibitor; Gram positive pathogens; Linezolid; Menaquinone biosynthesis inhibitor; Methicillin resistant Staphylococcus aureus; Peptide deformylase inhibitor; Peptidoglycan biosynthesis inhibitor; Phage therapy; Pol IIIC inhibitor; RNA polymerase inhibitor; Two component system inhibitor; Vancomycin

Indexed keywords

ANTIBIOTIC AGENT; BC 3205; BC 3781; BC 7013; BETA LACTAMASE INHIBITOR; CETHROMYCIN; DALBAVANCIN; DAPTOMYCIN; DELAFLOXACIN; DIHYDROFOLATE REDUCTASE INHIBITOR; ERAVACYCLINE; ICLAPRIM; LINEZOLID; MODITHROMYCIN; NXL 103; ORITAVANCIN; PEPTIDE DEFORMYLASE INHIBITOR; PROTEINASE INHIBITOR; PSEUDOMONIC ACID; RADEZOLID; TD 1792; TEDIZOLID; TOMOPENEM; UNCLASSIFIED DRUG; VANCOMYCIN; XF 73; XRP 2868;

ANTIMICROBIAL ACTIVITY; DRUG MECHANISM; DRUG SCREENING; GRAM POSITIVE INFECTION; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; PRIORITY JOURNAL; REVIEW; STAPHYLOCOCCUS INFECTION;

EID: 84882948283     PISSN: 17460441     EISSN: 1746045X     Source Type: Journal    
DOI: 10.1517/17460441.2013.807246     Document Type: Review

References (184)

1. Grenet K, Guillemot D, Jarlier V, et al. Antibacterial resistance, Wayampis Amerindians, French Guyana. Emerg Infect Dis 2004;10:1150-4
2. Cosgrove SE, Fowler VG. Management of methicillin-resistant Staphylococcus aureus bacteremia. Clin Infect Dis 2008;46:S386-93 (Pubitemid 351717326)
3. Cunha BA. Vancomycin revisited: A reappraisal of clinical use. Crit Care Clin 2008;24:393-420 (Pubitemid 351400623)
4. Loffler CA, Macdougall C. Update on prevalence and treatment of methicillin-resistant Staphylococcus aureus infections. Expert Rev Anti Infect Ther 2007;5:961-81 (Pubitemid 350303027)
5. Tacconelli E, Cataldo MA. Antimicrobial therapy of Staphylococcus aureus bloodstream infection. Exp Opin Pharmacother 2007;8:2505-18 (Pubitemid 350031290)
6. Klevens RM, Edwards JR, Tenover FC, et al. Changes in the epidemiology of methicillin-resistant Staphylococcus aureus in intensive care units in US hospitals, 1992-2003. Clin Infect Dis 2006;42:389-91 (Pubitemid 43122317)
7. Gaynes R, Edwards JR. Overview of nosocomial infections caused by Gram-negative bacilli. Healthcare Epidemiol 2005;41:848-54 (Pubitemid 41266753)
8. Kluytmans-Vabdenbergh MFQ, Kluytmans JAJW. Community-acquired methicillin-resistant Staphylococcus aureus: Current perspectives. Clin Microbial Infect. 2006;12:9-15
9. Klein E, Smith DL, Laxminarayan R. Hospitalizations and deaths caused by methicillin-resistant Staphylococcus aureus. United States, 1999-2005. Emerg Infect Dis 2007;13:1840-6
10. Eady EA, Cove JH. Staphylococcal resistance revisited: Community-acquired methicillin-resistant Staphylococcus aureus-an emerging problem for the management of skin and soft tissue infections. Curr Opin Infect Dis 2003;16:103-24 (Pubitemid 36521023)
11. Kaneko J, Kamio Y. Bacterial two-component and hetero-heptameric pore-forming cytolytic toxins: Structures, pore-forming mechanism, and organization of the genes. Biosci Biotechnol Biochem 2004;68:981-1003 (Pubitemid 39251411)
12. Lina G, Piémont Y, Godail-Gamot F. Involvement of Panton-Valentine leukocidin-producing Staphylococcus aureus in primary skin infections and pneumonia. Clin Infect Dis 1999;29:1128-32 (Pubitemid 30265628)
13. Diederen BMW, Kluytmans JAJW. The emergence of infections with community-associated methicillin resistant Staphylococcus aureus. J Infect 2006;52:157-68 (Pubitemid 43286181)
14. Barbachyn MR, Ford CW. Oxazolidinone structure-activity relationships leading to linezolid. Angew Chem Int Eng 2003;42:2010-23 (Pubitemid 36604340)
15. Wilcox MH. Update on linezolid: The first oxazolidinone antibiotic. Exp Opin Pharmacother 2005;6:2315-26 (Pubitemid 41582217)
16. Schentag JJ, Hyatt JM, Carr JR, et al. Genesis of methicillin-resistant Staphylococcus aureus (MRSA), how treatment of MRSA infections has selected for vancomycin-resistant Enterococcus faecium, and the importance of antibiotic management and infection control. Clin Infect Dis 1998;26:1204-14
17. Donadio S, Soiso M. Biosynthesis of glycopeptides: Prospects for improved antibacterials. Curr Top Med Chem 2008;8:654-66 (Pubitemid 351982573)
18. Pace JL, Yang G. Glycopeptides: Update on an old successful antibiotic class. Biochem Pharmacol 2006;71:968-80
19. Gales AC, Sader HS, Andrade SS, et al. Emergence of linezolid-resistant Staphylococcus aureus during treatment of pulmonary infection in patient with cystemic fibrosis. Int J Antimicro Agents 2007;27:300-2
20. Woodworth JR, Nyhart EH, Brier GL, et al. Single-dose pharmacokinetics and antibacterial activity of daptomycin, a new lipopeptide antibiotic, in healthy volunteers. Antimicrob Agents Chemother 1992;36:318-25
21. Henken S, Bohling J, Martens-Lobenhoffer M, et al. Efficacy profiles of daptomycin for treatment of invasive and noninvasive pulmonary infections with Streptococcus pneumonia. Antimicrob Agents Chemother 2010;54:707-17
22. Anthony KB, Fishman NO, Linkin DR, et al. Clinical and microbiological outcomes of serious infections with multidrug-resistant Gram-negative organisms treated with tigecycline. Clin Infect Dis 2008;46:567-70 (Pubitemid 351263497)
23. Boucher HW, Talbot GH, Bradley JS, et al. Bad bugs, no drugs: No ESKAPE! An update from the infectious diseases society of America. Clin Infect Dis 2009;48:1-12
24. Rybak MJ. The Pharmacokinetic and pharmacodynamic properties of vancomycin. Clin Infect Dis 2006;42:S35-9 (Pubitemid 41832063)
25. Robles-Piedras AL, González-Lòpez EH. Therapeutic drug monitoring of vancomycin. Proc West Pharmacol Soc 2009;52:21-3
26. Micek ST. Alternatives to vancomycin for the treatment of Methicillin-Resistant Staphylococcus aureus Infections. Clin Infect Dis 2007;45:S184-90 (Pubitemid 47378905)
27. Schmidt-Ioanas M, De Roux A, Lode H. New antibiotics for the treatment of severe staphylococcal infection in the critically ill patient. Curr Opin Crit Care 2005;11:481-6 (Pubitemid 41482705)
28. Rayner C, Munchhof WJ. Antibiotics currently used in the treatment of infections caused Staphylococcus aureus. Inter Med J 2005;35:S3-16 (Pubitemid 44933536)
29. Safety information of tigecycline. Available from: Http://www.fda.gov/ Safety/MedWatch/SafetyInformation/ SafetyAlertsforHumanMedicalProducts/ ucm224626.htm
30. Jacqueline C, Navans D, Batard E, et al. In vitro and in vivo synergistic activities of linezolid combined with subinhibitory concentrations of imipenem against methicillin-resistant Staphylococcus aureus. Antimicro Agents Chemother 2005;49:45-51 (Pubitemid 40065771)
31. Kollef MH. New antimicrobial agents for methicillin-resistant Staphylococcus aureus. Crit Care Resusc 2009;11:282-6
32. Kanafani ZA, Corey GR. Ceftaroline: A cephalosporin with expanded Gram-positive activity. Future Microbiol 2009;4:25-33
33. Steed ME, Rybak MJ. Ceftaroline: A new cephalosporin with activity against resistant Gram-positive pathogens. Pharmacotherapy 2010;30:375-89
34. Garci'a MS, Torre MA, Morales G, et al. Clinical outbreak of linezolid-resistant Staphylococcus aureus in an intensive care unit. JAMA 2010;303:2260-4
35. Saravolatz LD, Stein GE, Johnson LB. Telavancin: A novel lipoglycopeptide. Clin Infect Dis 2009;49:1908-14
36. Donadio S, Maffioli S, Monciardini P, et al. Antibiotic discovery in the twenty-first century: Current trends and future perspectives. J Antibiot 2010;63:423-30
37. Belley A, McKay GA, Arhin FF, et al. Oritavancin disrupts membrane integrity of Staphylococcus aureus and vancomycin-resistant enterococci to effect rapid bacterial killing. Antimicrob Agents Chemother 2010;54:5369-71
38. Zhanel GG, Schweizer F, Karlowsky JA. Oritavancin: Mechanism of action. Clini Infect Dis 2012;54:S214-19
39. Chen AY, Zervos MJ, Vazquez JA. Dalbavancin: A novel antimicrobial. Int J Clin Pract 2007;61:853-63 (Pubitemid 46587871)
40. Blais J, Lewis SR, Krause KM, et al. Antistaphylococcal activity of TD-1792, a multivalent glycopeptide-cephalosporin antibiotic. Antimicrob Agents Chemother 2012;56:1584-7
41. Leuthner KD, Vidaillac C, Cheung CM, et al. In vitro activity of the new multivalent glycopeptide-cephalosporin antibiotic TD-1792 against vancomycin-nonsusceptible Staphylococcus isolates. Antimicrob Agents Chemother 2010;54:3799-803
42. Hegde SS, Okusanya OO, Skinner R, et al. Pharmacodynamics of TD-1792, a novel glycopeptide-cephalosporin heterodimer antibiotic used against Gram-positive bacteria, in a neutropenic murine thigh model. Antimicrob Agents Chemother 2012;56:1578-83
43. Announcement of clinical efficacy of TD-1792. Available from: Http://www. evaluatepharma.com/Universal/View.aspx? type=Story&id=132180
44. Hughes J, Mellows G. Inhibition of isoleucyl-transfer ribonucleic acid synthetase in Escherichia coli by pseudomonic acid. Biochem J 1978;176:305-18 (Pubitemid 9060536)
45. Grare M, Dibama HM, Lafosse S, et al. Cationic compounds with activity against multidrug-resistant bacteria: Interest of a new compound compared with two older antiseptics, hexamidine and chlorhexidine. Clin Microbiol Infect 2010;16:432-8
46. Coates T, Bax R, Coates A. Nasal decolonization of Staphylococcus aureus with mupirocin: Strengths, weaknesses and future prospects. J Antimicrob Chemother 2009;64:9-15
47. Watanakunakorn C, Axelson C, Bota B, et al. Mupirocin ointment with and without chlorhexidine baths in the eradication of Staphylococcus aureus nasal carriage in nursing home residents. Am J Infect Control 1995;23:306-9
48. Schneider P, Hawser S, Islam K. Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria. Bioorg Med Chem Lett 2003;13:4217-21 (Pubitemid 37410316)
49. Morgan A, Cofer C, Stevens D. Iclaprim: A novel dihydrofolate reductase inhibitor for skin and soft tissue infections. Future Microbiol 2009;4:131-44
50. Peppard W, Schuenke C. Iclaprim, a diaminopyrimidine dihydrofolate reductase inhibitor for the potential treatment of antibiotic-resistant Staphylococcal infections. Curr Opin Investig Drugs 2008;9:210-25 (Pubitemid 351206380)
51. Kohlhoff S, Sharma R. Iclaprim. Expert Opin Investig Drugs 2007;16:1441-8
52. Available from: Http://clinicaltrials.gov/ show/NCT00543608
53. Ooi N, Miller K, Hobbs J, et al. XF-73, a novel antistaphylococcal membrane-active agent with rapid bactericidal activity. J Antimicrob Chemother 2009;64:735-40
54. Farrell DJ, Robbins M, Rhys-Williams W, et al. Investigation of the potential for mutational resistance to XF-73, retapamulin, mupirocin, fusidic acid, daptomycin, and vancomycin in methicillin-resistant Staphylococcus aureus isolates during a 55-passage study. Antmicro Agents Chemother 2011;55:1177-81
55. Kumar K, Chopra S. New drugs for methicillin-resistant Staphylococcus aureus: An update. J Antimicrob Chemother 2013;68:1-6
56. Grossman T, Starosta A, Fyfe C, et al. Target- and resistance-based mechanistic studies with TP-434, a novel fluorocycline antibiotic. Antimicrob Agents Chemother 2012;56:2559-64
57. Christ D, Sutcliffe J. TP-434 is Metabolically stable and has low potential for drug-drug interactions. Poster 181 F1-2162, 50th Annual ICAAC 2010. Available from: Http:// www.tphase.com/files/F1-2162.pdf
58. Horn PT, Sutcliffe JA, Walpole S, et al. Pharmacokinetics, safety and tolerability of a novel fluorocycline, TP-434, following multiple dose oral administration with and without food. IDSA Annual Meeting Boston, Poster Abstract Session; 2011
59. Sader H, Paukner S, Schoenfeld Z, et al. Antimicrobial activity of the novel pleuromutilin antibiotic BC-3781 against organisms responsible for community-acquired respiratory tract infections (CARTIs). J Antimicrob Chemother 2012;67:1170-5
60. Ross J, Sader H, Schoenfeld Z, et al. Disk diffusion and MIC quality control ranges for BC-3205 and BC-3781, two novel pleuromutilin antibiotics. J Clin Microbiol 2012;50:3361-4
61. Declaration of clinical research on BC-3781. Available from: Http://www. biotech-intelligence.com/html/html/ pool-7/ 88ba7b2fec852709f7c5df2e8fb3511e. html
62. Skripkin E, McConnell T, DeVito J, et al. RX-01, a New family of oxazolidinones that overcome ribosome-based linezolid resistance. Antimicrob Agents Chemother 2008;52:3550-7
63. Lawrence L, Danese P, DeVito J, et al. In vitro activities of the RX-01 oxazolidinones against hospital and community pathogens. Antimicrob Agents Chemother 2008;52:1653-62 (Pubitemid 351614657)
64. Zhou J, Bhattacharjee A, Chen S, et al. Design at the atomic level: Design of biaryloxazolidinones as potent orally active antibiotics. Bioorg Med Chem Lett 2008;18:6175-8
65. Available from: Http://www.clinicaltrials. gov/ct2/results?term=RX-1741 +&Search=Search
66. Louie A, Liu W, Kulawy R, et al. In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin- susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model. Antimicrob Agents Chemother 2011;55:3453-60
67. Brown SD, Traczewski MM. Comparative in vitro antimicrobial activities of torezolid (TR-700), the active moiety of a new oxazolidinone, torezolid phosphate (TR-701), determination of tentative disk diffusion interpretive criteria, and quality control ranges. Antimicrob Agents Chemother 2010;54:2063-9
68. Prokocimer P, Bien P, Surber J, et al. Phase 2, randomized, double-blind, dose-ranging study evaluating the safety, tolerability, population pharmacokinetics, and efficacy of oral torezolid phosphate in patients with complicated skin and skin structure infections. Antimicrob Agents Chemother 2011;55:583-92
69. Koga T, Masuda N, Kakuta M, et al. Potent in vitro activity of tomopenem (CS-023) against methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa. Antimicrob Agents Chemother 2008;52:2849-54
70. Tanka K, Mikamo H, Nakao K, et al. In vitro activity of tomopenem (CS-023/ RO4908463) against anaerobic bacteria. Antimicrob Agents Chemother 2009;53:319-22
71. Tomozawa T, Sugihara C, Kakuta M, et al. In vitro postantibiotic effects of tomopenem (CS-023) against Staphylococcus aureus and Pseudomonas aeruginosa. J Med Microbiol 2010;59:438-41
72. Sugihara K, Sugihara C, Matsushita Y, et al. In vivo pharmacodynamic activity of tomopenem (formerly CS-023) against Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus in a murine thigh infection model. Antimicrob Agents Chemother 2010;54:5298-302
73. Rios AM, Mejias R, Chavez-Bueno S, et al. Impact of cethromycin (ABT-773) therapy on microbiological, histologic, immunologic, and respiratory indices in a murine model of Mycoplasma pneumoniae lower respiratory infection. Antimicrob Agents Chemother 2004;48:2897-904 (Pubitemid 38989153)
74. Garcia I, Pascual A, Ballesta S, et al. Accumulation and activity of cethromycin (ABT-773) within human polymorphonuclear leucocytes. J Antimicrob Chemother 2003;52:24-8 (Pubitemid 36850080)
75. Kim MK, Zhou W, Tessier PR, et al. Bactericidal effect and pharmacodynamics of cethromycin (ABT-773) in a murine Pneumococcal pneumonia model. Antimicrob Agents Chemother 2002;46:3185-92
76. Bermudez LE, Motamedi N, Chee C, et al. EDP-420, a bicyclolide (bridged bicyclic macrolide), is active against Mycobacterium avium. Antimicrob Agents Chemother 2007;51:1666-70 (Pubitemid 46744143)
77. Luo X, Wu R, Wang M, et al. Comparative efficacy of EDP-420, azithromycin, telithromycin, clindamycin, trimethoprim/sulfamethoxazole, linezolid and levofloxacin against murine skin abscess induced by methicillin-resistant Staphylococcus aureus USA300 PVL+ mecA strain. 18th European Congress of Clinical Microbiology and Infectious Diseases; 2008
78. Paknikar SS, Narayana S. Newer antibacterials in therapy and clinical trial. North Am J Med Sci 2012;4:537-47
79. Xu G, Tang D, Gai Y, et al. An efficient large-scale synthesis of EDP-420, a First-in-class bridged bicyclic macrolide (BBM) antibiotic drug candidate. Org Proc Res Dev 2010;4:504-10
80. Pankuch GA, Kelly LM, Lin G, et al. Activities of a new oral streptogramin, XRP 2868, compared to those of other agents against Streptococcus pneumoniae and Haemophilus species. Antimicrob Agents Chemother 2003;47:3270-4 (Pubitemid 37229588)
81. Andes D, Craig WA. Pharmacodynamics of a new streptogramin, XRP 2868, in murine thigh and lung infection models. Antimicrob Agents Chemother 2006;50:243-9 (Pubitemid 43042928)
82. Mabe S, Champney WS. A comparison of a new oral streptogramin XRP 2868 with quinupristin-dalfopristin against antibiotic-resistant strains of Haemophilus influenzae, Staphylococcus aureus, and Streptococcus pneumoniae. Curr Microbiol 2005;51:363-6 (Pubitemid 41759131)
83. Goldstein E, Citron D, Merriam V, et al. Comparative in vitro Activities of XRP 2868, pristinamycin, quinupristin-dalfopristin, vancomycin, daptomycin, linezolid, clarithromycin, telithromycin, clindamycin, and ampicillin against anaerobic Gram-positive species, actinomycetes, and lactobacilli. Antimicrob Agents Chemother 2005;49:408-13
84. Lemaire S, Tulkens P, Van Bambeke F. Contrasting effects of acidic pH on the extracellular and intracellular activities of the anti-Gram-positive fluoroquinolones moxifloxacin and delafloxacin against Staphylococcus aureus. Antimicrob Agents Chemother 2011;55:649-58
85. Announcement of phase study results for delafloxacin. Available from: Http://www. rib-x.com/pipeline/delafloxacin.php
86. Jones RN, Sader HS, Fritsche TR. Antimicrobial activity of LBM415 (NVP PDF-713) tested against pathogenic Neisseria spp. (Neisseria gonorrhoeae and Neisseria meningitidis). Diagn Micr Infec Dis 2005;51:139-41 (Pubitemid 40215425)
87. Rolan P, Sun H, MacLeod C, et al. Pharmacokinetics and unexpected safety issues of LBM415, a novel oral peptide deformylase inhibitor. Clin Pharmacol Ther 2011;90:256-62
88. Bell JM, Turnidge JD, Inoue M, et al. Activity of a peptide deformylase inhibitor LBM415 (NVP PDF-713) tested against recent clinical isolates from Japan. J Antimicrob Chemother 2005;55:276-8 (Pubitemid 40331161)
89. Osborne CS, Neckermann G, Fischer E, et al. In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models. Antimicrob Agents Chemother 2009;53:3777-81
90. Ednie LM, Pankuch G, Appelbaum PC. antipneumococcal activity of LBM415, a new peptide diformylase inhibitor, compared with those of other agents. Antimicrob Agents Chemother 2004;48:4027-32 (Pubitemid 39304641)
91. Ross J, Scangarella-Oman N, Miller N, et al. Determination of disk diffusion and MIC quality control ranges for GSK1322322, a novel peptide deformylase inhibitor. J Clin Microbiol 2011;49:3928-30
92. Verma SK, Jat RK, Nagar N, et al. A novel antibacterial target: Peptide deformylase. Pharmacophore J 2011;2:114-23
93. Bogdanovich T, Smith KA, Clark C, et al. Activity of LBM415 compared to those of 11 other agents against Haemophilus species. Antimicrob Agents Chemother 2006;50:2323-9 (Pubitemid 43993169)
94. Gordon JY, Romanowski EG. A review of antimicrobial peptides and their therapeutic potential as anti-infective drugs. Curr Eye Res 2005;30:505-15 (Pubitemid 41113552)
95. Andres E, Dimarcq JL. Cationic antimicrobial peptides: Update of clinical development. J Intern Med 2004;255:519-20 (Pubitemid 38446366)
96. Hallock KJ, Lee D-K, Ramamoorthy A. MSI-78, an Analogue of the magainin antimicrobial peptides, disrupts lipid bilayer structure via positive curvature strain. Biophys J 2003;84:3052-60 (Pubitemid 36531755)
97. Available from: Www. dipexiumpharmaceuticals.com/ aboutLocilex.html
98. Rehm BHA. Microbial production of alginate: Biosynthesis and Applications in Microbial Production of Biopolymers and Polymer Precursors. 2009; Caister Academic Press. ISBN 978-1-904455-36- 3
99. Available from: Http://algipharma.no/ images/Marketing/News/Sept/ ICAAC-2012-poster-F-2062- AlgiPharmas-Oligo- G-bacterial-motility-study-at- CardiffU. pdf
100. Ebrt T, Smith S, Pancari G, et al. A fully human monoclonal antibody to Staphylococcus aureus iron regulated surface determinant B (IsdB) with functional activity in vitro and in vivo. Hum Antibodies 2010;19:113-28
101. Henck JO, Byrrn SR. Designing a molecular delivery system within a preclinical timeframe. Drug Discov Today 2007;12:189-99
102. Kelly-Quintos C, Cavacini LA, Posner MR, et al. Characterization of the opsonic and protective activity against Staphylococcus aureus of fully human monoclonal antibodies specific for the bacterial surface polysaccharide poly-N-acetylglucosamine. Infect Immun 2006;74:2742-50 (Pubitemid 43672983)
103. Kelly-Quintos C, Kropec A, Briggs S. The role of epitope specificity in the human opsonic antibody response to the Staphylococcal surface polysaccharide poly N-acetyl glucosamine. J Infect Dis 2005;192:2012-19 (Pubitemid 41681901)
104. Kutter E, De Vos D, Gvasalia G, et al. Phage therapy in clinical practice: Treatment of human infections. Curr Pharm Biotechnol 2010;11:69-86
105. Matsuzaki S, Rashel M, Uchiyama J, et al. Bacteriophage therapy: A revitalized therapy against bacterial infectious diseases. J Infect Chemother 2005;11:211-19 (Pubitemid 41570015)
106. Miedzybrodzki R, Fortuna W, Weber-Dabrowska B, et al. Phage therapy of staphylococcal infections (including MRSA) may be less expensive than antibiotic treatment. Postepy Hig Med Dosw 2007;61:461-5
107. Winter JM, Behnken S, Hertweck C. Genomics-inspired discovery of natural products. Curr Opin Chem Biol 2011;15:22-31
108. Goldstein BP, Berti M, Ripamonti F, et al. In vitro antimicrobial activity of a new antibiotic, MDL 62,879 (GE2270 A). Antimicrob Agents Chemother 1993;37:741-5 (Pubitemid 23096871)
109. Raja A, LaBonte J, Lebbos J, et al. Daptomycin. Nat Rev Drug Dis 2003;2:943-4 (Pubitemid 37540571)
110. Crowley PJ, Martini LG. Formulation design: New drugs from old. Drug Dis Today 2004;1:537-42 (Pubitemid 40197602)
111. LaMarche MJ, Leeds JA, Dzink-Fox J, et al. 4-aminothiazolyl analogues of GE2270 A: Antibacterial lead finding. J Med Chem 2011;54:2517-21
112. Ohlsen K. Novel antibiotics for the treatment of Staphylococcus aureus. Expert Rev Clin Pharmacol 2009;2:661-72
113. Roccaforte JS, Bittner MJ, Stumpf CA, et al. Attempts to eradicate methicillin-resistant Staphylococcus aureus colonization with the use of trimethoprim-sulfamethoxazole, rifampin, and bacitracin. Am J Infect Control 1988;16:141-6
114. Available from: Http://www.triusrx.com/ pdfs/Advanced-Microbiology-and- In- Vivo-Efficacy-of-Rx101005-a-Novel-2-4- Diaminoquinazoline-DHFR-Inhibitor.pdf
115. Mushtaq S, Warner M, Williams G, et al. Activity of chequerboard combinations of ceftaroline and NXL104 versus b-lactamase-producing Enterobacteriaceae. J Antimicrob Chemother 2010;65:1428-32
116. Xu H, Hazra S, Blanchard JS. NXL104 Irreversibly Inhibits the b-Lactamase from Mycobacterium tuberculosis. Biochemistry 2012;51:4551-7
117. Louie A, Castanheira M, Liu W, et al. Pharmacodynamics of b-lactamase inhibition by NXL104 in combination with ceftaroline: Examining organisms with multiple types of b-lactamases. Antimicrob Agents Chemother 2012;56:258-70
118. Wiskirchen DE, Crandon JL, Furtado GH, et al. In vivo efficacy of a human-simulated regimen of ceftaroline combined with NXL104 against extended-spectrum b-lactamase (ESBL)- producing and non-ESBL-producing Enterobacteriaceae. Antimicrob Agents Chemother 2011;55:3 220-5
119. Nafsika GH. b-Lactamase inhibitors: Evolving compounds for evolving resistance targets. Exp Opini Investig Drugs 2004;13:1307-18
120. Snydman DR, Jacobus NV, McDermott LA. Activity of a novel cyclic lipopeptide, CB-183,315, against resistant Clostridium difficile and other Gram-positive aerobic and anaerobic intestinal pathogens. Antimicrob Agents Chemother 2012;56:3448-52
121. Carmela MTM, Lawrence MI, Kare HT, et al. In vitro and in vivo characterization of CB-183,315, a novel lipopeptide antibiotic for treatment of Clostridium difficile. Antimicrob Agents Chemother 2012;56:5023-30
122. Mangili A, Bica I, Snydman DR, et al. Daptomycin-resistant, methicillin-resistant Staphylococcus aureus bacteremia. Clin Infect Dis 2005;40:1058-60 (Pubitemid 40418318)
123. Peleg AY, Miyakis S, Ward DV, et al. Whole genome characterization of the mechanisms of daptomycin resistance in clinical and laboratory derived isolates of Staphylococcus aureus. PLoS One 2012;7:e28316
124. Falagas ME, Grammatikos AP, Michalopoulos A. Potential of old-generation antibiotics to address current need for new antibiotics. Expert Rev Anti Infect Ther 2008;6:593-600
125. McLaws FB, Larsen AR, Skov RL, et al. Distribution of fusidic acid resistance determinants in methicillin-resistant Staphylococcus aureus. Antimicrob Agents Chemother 2011;55:1173-6
126. Br€otz-Oesterhelt H, Beyer D, Kroll HP, et al. Dysregulation of bacterial proteolytic machinery by a new class of antibiotics. Nat Med 2005;11:1082-7 (Pubitemid 41486830)
127. Li DHS, Chung YS, Gloyd M, et al. Acyldepsipeptide antibiotics induce the formation of a structured axial channel in ClpP: A model for the ClpX/ClpA-bound state of ClpP. Chem Biol 2010;17:959-69
128. Lee BG, Park EY, Lee KE, et al. Structures of ClpP in complex with acyldepsipeptide antibiotics reveal its activation mechanism. Nat Struct Mol Biol 2010;17:471-9
129. Hinzen B, Raddatz S, Paulsen H, et al. Medicinal chemistry optimization of acyldepsipeptides of the enopeptin class antibiotics. Chem Med Chem 2006;1:689-93 (Pubitemid 44154354)
130. Haste NM, Hughes CC, Tran DN, et al. Pharmacological properties of the marine natural product marinopyrrole A against methicillin-resistant Staphylococcus aureus. Antimicrob Agents Chemother 2011;55:3305-12
131. Doi K, Li R, Sung SS, et al. Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation. J Biol Chem 2012;287:10224-35
132. Nicolaou KC, Simmons NL, Chen JS, et al. Total synthesis and biological evaluation of marinopyrrole A and analogs. Tetrahedron Lett 2011;52:2041-3
133. Kwon YJ, Fang Y, Xu GH, et al. Aquastatin A, a new Inhibitor of enoyl-acyl carrier protein reductase from Sporothrix sp. FN611. Biol Pharm Bull 2009;32:2061-4
134. Yong K, Jayasuriya H, Ondeyka J, et al. Discovery of FabH/FabF inhibitors from natural products. Antimicrob Agents Chemother 2006;50:519-26 (Pubitemid 43190961)
135. Kithsiri HB, Hiranthi J, Ziqiang G, et al. Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents. J Nat Prod 2005;68:1437-40
136. Srinivas K, Andrew G, Katherine Y. Determination of selectivity and efficacy of fatty acid synthesis inhibitors. J Biol Chem 2005;280:1669-77
137. Zheng CJ, Sohn MJ, Kim WG. Vinaxanthone, a new FabI inhibitor from Penicillium sp. J Antimicrob Chemother 2009;63:949-53
138. Wang J, Kodali S, Lee SH, et al. Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties. Proc Natl Acad Sci USA 2007;104:7612-16 (Pubitemid 47185954)
139. Evan M, Arnold DL. Platensimycin and platencin: Promising antibiotics for future application in human medicine. J Antibiot 2011;64:705-10
140. Kato A, Nakaya S, Kokubo N, et al. A new anti-MRSA antibiotic complex, WAP-8294A I. Taxonomy, isolation and biological activities. J Antibiot 1998;51:929-35 (Pubitemid 28505287)
141. Hyeon-Hee Y, Kang-Ju K, Jeong-Dan C, et al. Antimicrobial activity of berberine alone and in combination with ampicillin or oxacillin against methicillin-resistant Staphylococcus aureus. J Med Food 2005;8:454-61
142. Bonner DP, O'Sullivan J, Tanaka KS, et al. Lysobactin, a novel antibacterial agent produced by Lysobacter sp. II. Biological properties. J Antibiot 1988;41:1745-51 (Pubitemid 19010340)
143. Franz N, Sonja A, Jordi B-B, et al. Structure and total synthesis of lysobactin (katanosin B). Angew Chem Int Ed 2007;46:2039-42
144. Hall EA, Kuru E, VanNieuwenhze MS. Solid-phase synthesis of lysobactin (katanosin B): Insights into structure and function. Org Lett 2012;14:2730-3
145. Zheng CJ, Yu HE, Kim EH, et al. Viridicatumtoxin B, a new anti-MRSA agent from Penicillium sp. FR11. J Antibiot 2008;61:633-7
146. Ma X-C, Sun C, Huang S-S, et al. Preparative isolation and purification of four prenylflavanones from microbial biotransformation of kurarinone by high-speed counter-current chromatography. Separ Puri Technol 2010;76:140-5
147. McDonald LA, Barbieri LR, Carter GT, et al. Structures of muraymycins, novel peptidoglycan biosynthesis inhibitors. J Am Chem Soc 2002;124:10260-1 (Pubitemid 34977365)
148. Lin YI, Li Z, Francisco GD, et al. Muraymycins, novel peptidoglycan biosynthesis inhibitors: Semisynthesis and SAR of their derivatives. Bioorg Med Chem Lett 2002;12:1341-4
149. Bouhss A, Crouvoisier M, Blanot D, et al. Purification and characterization of the bacterial MraY translocase catalyzing the first membrane step of peptidoglycan biosynthesis. J Biol Chem 2004;279:29974-80 (Pubitemid 38937917)
150. Silver LL. Does the cell wall of bacteria remain a viable source of targets for novel antibiotics? Biochem Pharmacol 2006;71:996-1005
151. Dini C. MraY inhibitors as novel antibacterial agents. Curr Topics Med Chem 2005;5:1221-36 (Pubitemid 43009756)
152. Aleiwi BA, Schneider CM, Kurosu M. Synthesis of ureidomuraymycidine derivatives for structure-activity relationship studies of muraymycins. J Org Chem 2012;77:3859-67
153. Winn M, Goss JM, Kimura K, et al. Antimicrobial nucleoside antibiotics targeting cell wall assembly: Recent advances in structure-function studies and nucleoside biosynthesis. Nat prod Rep 2010;27:279-304
154. Konishi M, Sugawara K, Hanada M, et al. Empedopeptin (BMY-28117), a new depsipeptide antibiotic. I. Production, isolation and properties. J Antibiot 1984;37:949-57 (Pubitemid 14033921)
155. Müller A, Münch D, Schmidt Y, et al. Lipodepsipeptide empedopeptin inhibits cell wall biosynthesis through Ca2 +-dependent complex formation with peptidoglycan precursors. J Biol Chem 2012;287:20270-80
156. Vértesy L, Aretz W, Knauf M, et al. Feglymycin, a novel inhibitor of the replication of the human immunodeficiency virus. Fermentation, isolation and structure elucidation. J Antibiot 1999;52:374-82 (Pubitemid 29213529)
157. Dettner F, Hänchen A, Schols D, et al. Total synthesis of the antiviral peptide antibiotic feglymycin. Angew Chem Int Ed 2009;48:1856-61
158. Rausch S, Hänchen A, Denisiuk A, et al. Feglymycin is an inhibitor of the enzymes MurA and MurC of the peptidoglycan biosynthesis pathway. Chem Bio Chem 2011;12:1171-3
159. Uchida R, Iwatsuki M, Kim YP, et al. Nosokomycins, new antibiotics discovered in an in vivo-mimic infection model using silkworm larvae. I: Fermentation, isolation and biological properties. J Antibiot 2010;63:151-5
160. Wyatt EE, Galloway WRJD, Thomas GL, et al. Identification of an anti-MRSA dihydrofolate reductase inhibitor from a diversity-oriented synthesis. Chem Commun 2008;44:4962-4
161. DaCunha EFF, Ramalho TC, Maia ER, et al. The search for new DHFR inhibitors: A review of patents January 2001-February 2005. Exp Opin Ther Patents 2005;15:967-86
162. Hawser S, Lociuro S, Islam K. Dihydrofolate reductase inhibitors as antibacterial agents. Biochem Pharmacol 2006;71:941-8
163. Karatas H, Alp M, Yildiz S, et al. Synthesis and potent in vitro activity of novel 1H-benzimidazoles as anti-MRSA agents. Chem Biol Drug Des 2012;80:237-44
164. Kurosu M, Begari E. Bacterial protein kinase inhibitors. Drug Dev Res 2010;71:168-87
165. Kurosu M, Begari E. Vitamin K2 in electron transport system: Are enzymes involved in vitamin K2 biosynthesis promising drug targets? Molecules 2010;15:1531-53
166. Kurosu M, Narayanasamy P, Biswas K, et al. Discovery of 1,4-dihydroxy-2- naphthoate prenyltransferase inhibitors: New drug leads for multidrug-resistant Gram-positive pathogens. J Med Chem 2007;50:3973-4
167. Debnath J, Siricilla S, Wan B, et al. Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis. J Med Chem 2012;55:3739-55
168. Dhiman RK, Mahapatra S, Slayden RA, et al. Menaquinone synthesis is critical for maintaining Mycobacterial viability during exponential growth and recovery from non-replicating persistence. Mol Microbiol 2009;72:85-97
169. Kashyap A, Sehgal VN, Sahu A, et al. Anti-leprosy drugs inhibit the complement-mediated solubilization of pre-formed immune complexes in vitro. Int J Immunopharmacol 1992;14:269-73
170. Yano T, Kassovska-Bratinova S, The JS, et al. Reduction of clofazimine by mycobacterial type 2 NADH:quinone oxidoreductase A. Pathway for the generation of bacterial levels of reactive oxygen species. J Biol Chem 2011;286:10276-87
171. Kuhl A, Svenstrup N, Ladel C. Biological characterization of novel inhibitors of the Gram-positive DNA polymerase IIIC enzyme. Antimicro Agents Chemother 2005;49:987-95 (Pubitemid 40327714)
172. Lee TX, Packer MD, Huang J, et al. Growth inhibitory and anti-tumour activities of OSU-03012, a novel PDK-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. Eur J Cancer 2009;45:1709-20
173. Chiua H-C, Leeb S-L, Kapuriya N. Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus. Bioorg Med Chem 2012;15:4653-60
174. Burton DC, Edwards JR, Horan TC, et al. Methicillin-resistant Staphylococcus aureus central line-associated bloodstream infections in us intensive care units, 1997-2007. J Am Med Associ 2009;301:727-36
175. Bush LM. Best alternative to vancomycin for serious methicillin-resistant Staphylococcus aureus infections: Let's just say it. Clin Infect Dis 2011;53:965-6
176. Pexer JC, Tancrede C, Tancrede D. In vitro study of the bactericidal activity of a sulfamethoxazole-trimethoprim combination of 59 hospital strains. Therapie 1970;25:13-28
177. Schiraldi O, Sforza E, Piaia F. Effect of a new sulfa-trimethoprim combination (trimethoprim -sulfamethopyrazine) in typhoid fever. A double-blind study on 72 adult patients. Chemotherapy 1985;31:68-75 (Pubitemid 15184160)
178. Bohni E. Comparative bacteriological investigations with the combination trimethoprim/sulfamethoxazole in vitro and in vivo. Chemotherapy 1969;14:1-21
179. Miyamoto E. Oral trimethoprim-sufamethoxazole for methicillin-resistant Staphylococcus aureus infections: The evidence behind the use. Drug Ther Topics 2004;33:69-74
180. Graham S, Coote PJ. Potent, synergistic inhibition of Staphylococcus aureus upon exposure to a combination of the endopeptidase lysostaphin and the cationic peptide ranalexin. J Antimicrob Chemother 2007;59:759-62 (Pubitemid 47073414)
181. Soeda H. Pharmacokinetics and therapeutic drug monitoring of anti-MRSA drugs. Kagaku Ryoho no Ryoiki 2011;28:1702-8
182. Chaudhary M, Shrivastava SM, Saurabh S, et al. In vitro antimicrobial activity of cefepime, amikacin and their fixed dose combination against some pathogenic bacteria. J Ecophysiol Occup Health 2008;8:161-5
183. Neu HC. Antibiotics in the second half of the 1980s. Areas of future development and the effect of new agents on aminoglycoside use. Am J Med 1986;80:195-203 (Pubitemid 16036788)
184. Bagnoli F, Bertholet S, Grandi G. Inferring reasons for the failure of Staphylococcus aureus vaccines in clinical trials. Front Cell Infect Microbiol 2012;2:16