New classes of antibiotics

Current Opinion in Pharmacology

Volumn 12, Issue 5, 2012, Pages 535-544

  Moir, Donald T ^a   Opperman, Timothy J ^a   Butler, Michelle M ^a   Bowlin, Terry L ^a  

^a MICROBIOTIX INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6,7 DIHYDRO 2 NITRO 6 (4 TRIFLUOROMETHOXYBENZYLOXY) 5H IMIDAZO[2,1 B][1,3]OXAZINE; ACTINONIN; AFN 1252; ANTIBIOTIC AGENT; BEDAQUILINE; BENZOFURAN DERIVATIVE; CG 400549; DELAMANID; DNA TOPOISOMERASE INHIBITOR; FAB 001; GENTAMICIN; GSK 1322322; GSK 2140944; GSK 2251052; MOLECULAR SCAFFOLD; N (5 FLUORO 1 OXIDO 2 PYRIDINYL) 1 [2 (N FORMYL N HYDROXYAMINOMETHYL)HEXANOYL]PROLINAMIDE; N [1 TERT BUTYL 2 OXO 2 [4 (2 THIAZOLYLMETHYL) 1 PIPERAZINYL]ETHYL] 3 CYCLOPENTYL 2 (N FORMYL N HYDROXYAMINOMETHYL)PROPIONAMIDE; PEPTIDE DEFORMYLASE INHIBITOR; PEPTIDOMIMETIC AGENT; PLACEBO; POL 7001; POL 7080; PORPHYRIN DERIVATIVE; RIFATER; TAVABOROLE; TRICLOSAN; TRICLOSAN DERIVATIVE; UNCLASSIFIED DRUG; XF 73;

ABDOMINAL INFECTION; ACUTE BACTERIA SKIN AND SKIN STRUCTURE INFECTION; ACUTE BACTERIAL SKIN AND SKIN STRUCTURE INFECTION; ANTIBIOTIC RESISTANCE; AREA UNDER THE CURVE; CLINICAL STUDY; COMMUNITY ACQUIRED BACTERIAL PNEUMONIA; COMMUNITY ACQUIRED PNEUMONIA; COMPLICATED BACTERIAL AND SKIN AND SKIN STRUCTURE INFECTION; COMPLICATED BACTERIAL SKIN AND SKIN STRUCTURE INFECTION; DRUG CLASSIFICATION; DRUG CLEARANCE; DRUG DOSE ESCALATION; DRUG EXCRETION; DRUG HALF LIFE; DRUG RESISTANT TUBERCULOSIS; DRUG STRUCTURE; DRUG TARGETING; GRAM NEGATIVE INFECTION; HUMAN; LUNG INFECTION; MAXIMUM PLASMA CONCENTRATION; MULTIDRUG RESISTANT TUBERCULOSIS; MYCOBACTERIUM; NONHUMAN; PRIORITY JOURNAL; PSEUDOMONAS; PSEUDOMONAS INFECTION; RESPIRATORY TRACT INFECTION; REVIEW; SEPTICEMIA; SKIN INFECTION; STAPHYLOCOCCUS; STAPHYLOCOCCUS INFECTION; STREPTOCOCCUS INFECTION; TUBERCULOSIS; URINARY TRACT INFECTION;

ANIMALS; ANTI-BACTERIAL AGENTS; CLINICAL TRIALS AS TOPIC; HUMANS;

EID: 84867330177     PISSN: 14714892     EISSN: 14714973     Source Type: Journal    
DOI: 10.1016/j.coph.2012.07.004     Document Type: Review

References (53)

1. J.A. Robinson, S.C. Shankaramma, P. Jetter, U. Kienzl, R.A. Schwendener, J.W. Vrijbloed, and D. Obrecht Properties and structure-activity studies of cyclic beta-hairpin peptidomimetics based on the cationic antimicrobial peptide protegrin I Bioorg Med Chem 13 2005 2055 2064
2. S.C. Shankaramma, Z. Athanassiou, O. Zerbe, K. Moehle, C. Mouton, F. Bernardini, J.W. Vrijbloed, D. Obrecht, and J.A. Robinson Macrocyclic hairpin mimetics of the cationic antimicrobial peptide protegrin I: a new family of broad-spectrum antibiotics Chembiochem 3 2002 1126 1133
3. N. Srinivas, P. Jetter, B.J. Ueberbacher, M. Werneburg, K. Zerbe, J. Steinmann, B. Van der Meijden, F. Bernardini, A. Lederer, and R.L. Dias Peptidomimetic antibiotics target outer-membrane biogenesis in Pseudomonas aeruginosa Science 327 2010 1010 1013
4. S. Wilbraham, S. DeMarco, A. Ograbek, J. Agren, A. Wach, D. Obrecht, and K. Demkowski Phase I study with the novel Pseudomonas aeruginosa antibiotic POL7080 in healthy volunteers 21st European Congress of Clinical Microbiology and Infectious Diseases (ECCMID), 27th International Congress if Chemotherapy (ICC) May 7-10 2011
5. V. Hernandez, T. Akama, M. Alley, S. Baker, W. Mao, F. Rock, Y.K. Zhang, Y. Zhou, T. Crepin, and S. Cusack Discovery and mechanism of action of AN3365: a novel boron containing antibacterial agent in clinical development for Gram-negative infections Poster F1-1637. 51st Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 17-20 2011
6. F.L. Rock, W. Mao, A. Yaremchuk, M. Tukalo, T. Crepin, H. Zhou, Y.K. Zhang, V. Hernandez, T. Akama, and S.J. Baker An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site Science 316 2007 1759 1761
7. D.J. Biedenbach, R.E. Mendes, M.R.K. Alley, H.S. Sader, and R.N. Jones Potency and spectrum of activity of AN3365, a novel boron-containing protein synthesis inhibitor, tested against non-fermentative Gram-negative Bacilli Poster F1-1639. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
8. S.K. Bouchillon, M.A. Hackel, D.J. Hoban, S.P. Hawser, and N.E. Scangarella-Oman GSK2251052, a novel boron-containing protein synthesis inhibitor, with comparative in vitro activity against Pseudomonas aeruginosa from a global population Poster E-129. 51st Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 17-20 2011
9. S.K. Bouchillon, D.J. Hoban, M.A. Hackel, D.L. Butler, P. Memarsh, and M.R.K. Alley In vitro activities of AN3365: a novel boron-cantaining protein synthesis inhibitor, and other antimicrobial agents against anaerobes and Neisseria Gonorrhoeae Neisseria Gonorrhoeae. Poster F1-1640. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
10. Y.R. Freund, L. Liu, M.R.K. Alley, W. Bu, S. Baker, S. Lux, A. O'Leary, and J.J. Plattner Murine pharmacokinetics and in vivo Gram-negative activity of AN3365: a novel boron-containing protein synthesis inhibitor Poster F1-1641. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
11. J. Hoover, C. Mininger, and S. Rittenhouse Dose ranging studies with the LeuRS inhibitor GSK2251052 against Escherichia coli in a mouse thigh suture infection model Poster A2-039. 51st Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 17-20 2011
12. L. Liu, S.J. Baker, M. Fitzsimmons, A. Watney, W. Bu, M. Potchoiba, M. Qi, V. Hernandez, M.R.K. Alley, and L. Feng Metabolic fate and disposition of GSK2251052, a novel boron-based antimicrobial against Gram-negative bacteria, in Sprague Dawley rats and cynomolgus monkeys 17th North American Regional ISSX 2011 ISSX Atlanta, GA, USA (Abstract P84)
13. L.T. Zane, S. Shakib, R. Milne, L. Liu, S.J. Baker, and F.A. Heerinckx Safety, tolerability, and pharmacokinetics of a novel Gram-negative antimicrobial, GSK2251052, in healthy subjects 21st European Congress of Clinical Microbiology and Infectious Diseases (ECCMID), 27th International Congress if Chemotherapy (ICC) May 7-10 2011
14. B.D. Bax, P.F. Chan, D.S. Eggleston, A. Fosberry, D.R. Gentry, F. Gorrec, I. Giordano, M.M. Hann, A. Hennessy, and M. Hibbs Type IIA topoisomerase inhibition by a new class of antibacterial agents Nature 466 2010 935 940
15. T.J. Miles, J.M. Axten, C. Barfoot, G. Brooks, P. Brown, D. Chen, S. Dabbs, D.T. Davies, D.L. Downie, and S. Eyrisch Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases Bioorg Med Chem Lett 21 2011 7489 7495
16. T.J. Miles, C. Barfoot, G. Brooks, P. Brown, D. Chen, S. Dabbs, D.T. Davies, D.L. Downie, S. Eyrisch, and I. Giordano Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases Bioorg Med Chem Lett 21 2011 7483 7488
17. K.W. Johnson, D. Lofland, and H.E. Moser PDF inhibitors: an emerging class of antibacterial drugs Curr Drug Targets Infect Disord 5 2005 39 52
18. P. Rolan, H. Sun, C. Macleod, K. Bracken, and T.G. Evans Pharmacokinetics and unexpected safety issues of LBM415, a novel oral peptide deformylase inhibitor Clin Pharmacol Ther 90 2011 256 262
19. D. Qin, Y. Fang, A. Benowitz, X. Liao, J. Karpinski, J. Dreabit, A. Knox, S. Kelly, J. Axten, and D. Mercer Peptide deformylase inhibitors: discovery of a clinical candidate from a novel chemical class Poster F1-2111. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
20. S. Bouchillon, M. Hackle, D. Hoban, M. Zalacain, and D. Butler In vitro activity of GSK1322322, a novel peptide deformylase inhibitor, against 4,836 pathogens from skin and soft tissue infections and respiratory tract infections Poster F1-2112. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
21. T. Lewandowski, P. Demarsh, T. Peters, and S. Kulkarni Potent activity of GSK1322322 a novel peptide deformylase inhibitor after oral dosing in a murine multi-drug resistant staphylococcus aureus infection model Poster F1-2113. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
22. C.M. Singley, J. Hoover, P. Demarsh, P. Elefante, and M. Zalacain Efficacy of GSK1322322 against Staphylococcus aureus in a Rat Subcutaneous Abscess Model Using a Human Exposure Profile Poster F1-2114. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
23. T. Lewandowski, T. Peters, N. Simon, and S. Kulkarni Potent activity of GSK1322322 a novel peptide deformylase inhibitor in a Haemophilus influenzae and Streptococcus pneumoniae respiratory tract infection model Poster F1-2115. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
24. N. Kaplan, and B. Hafkin Tolerability, safety and pharmacokinetics of multiple oral doses of AFN-1252 in healthy subjects Poster F1-1349. 51st Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 17-20 2011
25. H. Lu, and P.J. Tonge Inhibitors of FabI, an enzyme drug target in the bacterial fatty acid biosynthesis pathway Acc Chem Res 41 2008 11 20
26. D.J. Payne, W.H. Miller, V. Berry, J. Brosky, W.J. Burgess, E. Chen, W.E. DeWolf Jr., A.P. Fosberry Jr., R. Greenwood, and M.S. Head Discovery of a novel and potent class of FabI-directed antibacterial agents Antimicrob Agents Chemother 46 2002 3118 3124
27. J.B. Parsons, M.W. Frank, C. Subramanian, P. Saenkham, and C.O. Rock Metabolic basis for the differential susceptibility of Gram-positive pathogens to fatty acid synthesis inhibitors Proc Natl Acad Sci U S A 108 2011 15378 15383
28. J.A. Karlowsky, N.M. Laing, T. Baudry, N. Kaplan, D. Vaughan, D.J. Hoban, and G.G. Zhanel In vitro activity of API-1252, a novel FabI inhibitor, against clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis Antimicrob Agents Chemother 51 2007 1580 1581
29. J.A. Karlowsky, N. Kaplan, B. Hafkin, D.J. Hoban, and G.G. Zhanel AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity Antimicrob Agents Chemother 53 2009 3544 3548
30. W.J. Weiss, B. Hafkin, N. Kaplan, M. Pulse, P. Nguyen, P. Renick, and J. Simecka Oral pharmacokinetics and efficacy of AFN-1252 in a murine septicemia infection model with S. aureus Poster F1-833. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
31. L.M. McMurry, M. Oethinger, and S.B. Levy Triclosan targets lipid synthesis Nature 394 1998 531 532
32. R.J. Heath, Y.T. Yu, M.A. Shapiro, E. Olson, and C.O. Rock Broad spectrum antimicrobial biocides target the FabI component of fatty acid synthesis J Biol Chem 273 1998 30316 30320
33. M.A. Seefeld, W.H. Miller, K.A. Newlander, W.J. Burgess, W.E. DeWolf Jr., P.A. Elkins, M.S. Head, D.R. Jakas, C.A. Janson, and P.M. Keller Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK J Med Chem 46 2003 1627 1635
34. S. Escaich, L. Prouvensier, M. Saccomani, L. Durant, M. Oxoby, V. Gerusz, F. Moreau, V. Vongsouthi, K. Maher, and I. Morrissey The MUT056399 inhibitor of FabI is a new antistaphylococcal compound Antimicrob Agents Chemother 55 2011 4692 4697
35. T. Bogdanovich, C. Clark, K. Kosowska-Shick, B. Dewasse, P. McGhee, and P.C. Appelbaum Antistaphylococcal activity of CG400549, a new experimental FabI inhibitor, compared with that of other agents Antimicrob Agents Chemother 51 2007 4191 4195
36. N. Ooi, K. Miller, J. Hobbs, W. Rhys-Williams, W. Love, and I. Chopra XF-73, a novel antistaphylococcal membrane-active agent with rapid bactericidal activity J Antimicrob Chemother 64 2009 735 740
37. D.J. Farrell, M. Robbins, W. Rhys-Williams, and W.G. Love In vitro activity of XF-73, a novel antibacterial agent, against antibiotic-sensitive and -resistant Gram-positive and Gram-negative bacterial species Int J Antimicrob Agents 35 2010 531 536
38. N. Ooi, K. Miller, C. Randall, W. Rhys-Williams, W. Love, and I. Chopra XF-70 and XF-73, novel antibacterial agents active against slow-growing and non-dividing cultures of Staphylococcus aureus including biofilms J Antimicrob Chemother 65 2010 72 78
39. W.G. Love, I. Hayter, W. Rhys-Williams, G. Webb, and E.S. Johnson A Phase I study to determine safety, tolerability and preliminary anti-staphylococcal activity of intranasally administered XF-73 Poster K-307. 50th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) September 12-15 2010
40. C.E. Barry 3rd Unorthodox approach to the development of a new antituberculosis therapy N Engl J Med 360 2009 2466 2467
41. K. Andries, P. Verhasselt, J. Guillemont, H.W. Gohlmann, J.M. Neefs, H. Winkler, J. Van Gestel, P. Timmerman, M. Zhu, and E. Lee A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis Science 307 2005 223 227
42. A. Koul, N. Dendouga, K. Vergauwen, B. Molenberghs, L. Vranckx, R. Willebrords, Z. Ristic, H. Lill, I. Dorange, and J. Guillemont Diarylquinolines target subunit c of mycobacterial ATP synthase Nat Chem Biol 3 2007 323 324
43. A.C. Haagsma, R. Abdillahi-Ibrahim, M.J. Wagner, K. Krab, K. Vergauwen, J. Guillemont, K. Andries, H. Lill, A. Koul, and D. Bald Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue Antimicrob Agents Chemother 53 2009 1290 1292
44. S.P. Rao, S. Alonso, L. Rand, T. Dick, and K. Pethe The protonmotive force is required for maintaining ATP homeostasis and viability of hypoxic, nonreplicating Mycobacterium tuberculosis Proc Natl Acad Sci U S A 105 2008 11945 11950
45. A.H. Diacon, A. Pym, M. Grobusch, R. Patientia, R. Rustomjee, L. Page-Shipp, C. Pistorius, R. Krause, M. Bogoshi, and G. Churchyard The diarylquinoline TMC207 for multidrug-resistant tuberculosis N Engl J Med 360 2009 2397 2405
46. U. Manjunatha, H.I. Boshoff, and C.E. Barry The mechanism of action of PA-824: Novel insights from transcriptional profiling Commun Integr Biol 2 2009 215 218
47. M. Matsumoto, H. Hashizume, T. Tomishige, M. Kawasaki, H. Tsubouchi, H. Sasaki, Y. Shimokawa, and M. Komatsu OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice PLoS Med 3 2006 e466
48. R. Singh, U. Manjunatha, H.I. Boshoff, Y.H. Ha, P. Niyomrattanakit, R. Ledwidge, C.S. Dowd, I.Y. Lee, P. Kim, and L. Zhang PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release Science 322 2008 1392 1395
49. C.K. Stover, P. Warrener, D.R. VanDevanter, D.R. Sherman, T.M. Arain, M.H. Langhorne, S.W. Anderson, J.A. Towell, Y. Yuan, and D.N. McMurray A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis Nature 405 2000 962 966
50. R. Tasneen, S. Tyagi, K. Williams, J. Grosset, and E. Nuermberger Enhanced bactericidal activity of rifampin and/or pyrazinamide when combined with PA-824 in a murine model of tuberculosis Antimicrob Agents Chemother 52 2008 3664 3668
51. A.H. Diacon, R. Dawson, M. Hanekom, K. Narunsky, A. Venter, N. Hittel, L.J. Geiter, C.D. Wells, A.J. Paccaly, and P.R. Donald Early bactericidal activity of delamanid (OPC-67683) in smear-positive pulmonary tuberculosis patients Int J Tuberc Lung Dis 15 2011 949 954
52. A.H. Diacon, R. Dawson, M. Hanekom, K. Narunsky, S.J. Maritz, A. Venter, P.R. Donald, C. van Niekerk, K. Whitney, and D.J. Rouse Early bactericidal activity and pharmacokinetics of PA-824 in smear-positive tuberculosis patients Antimicrob Agents Chemother 54 2010 3402 3407
53. A.M. Ginsberg, M.W. Laurenzi, D.J. Rouse, K.D. Whitney, and M.K. Spigelman Safety, tolerability, and pharmacokinetics of PA-824 in healthy subjects Antimicrob Agents Chemother 53 2009 3720 3725