Mycobacterium tuberculosis: Drug resistance and future perspectives

Future Microbiology

Volumn 4, Issue 5, 2009, Pages 597-614

  Riccardi, Giovanna ^a   Pasca, Maria Rosalia ^a   Buroni, Silvia ^a  

^a UNIVERSITY OF PAVIA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1 (6 BROMO 2 METHOXY 3 QUINOLINYL) 4 DIMETHYLAMINO 2 (1 NAPHTHYL) 1 PHENYL 2 BUTANOL; 2,3 DIHYDRO 2 METHYL 6 NITRO 2 [4 [4 (4 TRIFLUOROMETHOXYPHENOXY) 1 PIPERIDINYL]PHENOXYMETHYL]IMIDAZO[2,1 B]OXAZOLE; 6,7 DIHYDRO 2 NITRO 6 (4 TRIFLUOROMETHOXYBENZYLOXY) 5H IMIDAZO[2,1 B][1,3]OXAZINE; AMIKACIN; AMINOGLYCOSIDE ANTIBIOTIC AGENT; AMINOSALICYLIC ACID; AMPICILLIN; CHLORAMPHENICOL; CYCLOSERINE; ETHAMBUTOL; ETHIONAMIDE; GATIFLOXACIN; ISONIAZID; KANAMYCIN; LEVOFLOXACIN; LINEZOLID; MOXIFLOXACIN; N (2 ADAMANTYL) N' GERANYLETHYLENEDIAMINE; NEOMYCIN; PYRAZINAMIDE; QUINOLINE DERIVED ANTIINFECTIVE AGENT; RIFABUTIN; RIFAMPICIN; RIFAMYCIN; RIFAPENTINE; STREPTOMYCIN; TETRACYCLINE; TOBRAMYCIN; UNINDEXED DRUG; VANCOMYCIN;

ANTIBIOTIC RESISTANCE; ANTIBIOTIC SENSITIVITY; BACTERIAL GENETICS; BACTERIAL TRANSMISSION; BACTERICIDAL ACTIVITY; BACTERIOSTASIS; CLINICAL TRIAL; DIRECTLY OBSERVED THERAPY; DRUG EFFICACY; DRUG STRUCTURE; DRUG TARGETING; EXTRAPULMONARY TUBERCULOSIS; GENE MUTATION; HUMAN; LUNG TUBERCULOSIS; MINIMUM INHIBITORY CONCENTRATION; MULTIDRUG RESISTANCE; MYCOBACTERIUM TUBERCULOSIS; NONHUMAN; OTOTOXICITY; PRIORITY JOURNAL; REVIEW; TUBERCULOSIS; TUBERCULOSIS CONTROL;

ANTITUBERCULAR AGENTS; BIOMEDICAL RESEARCH; DRUG RESISTANCE, BACTERIAL; HUMANS; MYCOBACTERIUM TUBERCULOSIS; TUBERCULOSIS;

MYCOBACTERIUM TUBERCULOSIS;

EID: 67149118143     PISSN: 17460913     EISSN: None     Source Type: Journal    
DOI: 10.2217/fmb.09.20     Document Type: Review

References (124)

1. Bhatt K, Salgame P: Host innate immune response to Mycobacterium tuberculosis. J. Clin. Immunol. 27(4), 347-362 (2007).
2. Saunders BM, Britton WJ: Life and death in the granuloma: immunopathology of tuberculosis. Immunol. Cell Biol. 85(2), 103-111 (2007).
3. Russell DG: Who puts the tubercle in tuberculosis' Nat Rev Microbiol. 5(1), 39-47 (2007).
4. Davis JM, Ramakrishnan L: The role of the granuloma in expansion and dissemination of early tuberculous infection. Cell 136(1), 37-49 (2009).
5. Lin MY, Ottenhoff TH: Host-pathogen interactions in latent Mycobacterium tuberculosis infection: identification of new targets for tuberculosis intervention. Endocr. Metab. Immune Disord. Drug Targets 8(1), 15-29 (2008).
6. El-Sadr WM, Tsiouris SJ: HIV-associated tuberculosis: diagnostic and treatment challenges. Semin. Respir. Crit. Care Med. 29(5), 525-531 (2008).
7. Chakrabarti B, Davies PD: Key issues in multidrug-resistant tuberculosis. Future Microbiol. 2, 51-61 (2007).
8. Maartens G, Wilkinson RJ: Tuberculosis. Lancet 370(9604), 2030-2043 (2007).
9. Goldman RC, Plumley KV, Laughon BE: The evolution of extensively drug resistant tuberculosis (XDR-TB): history, status and issues for global control. Infect. Disord. Drug Targets 7(2), 73-91 (2007).
10. Chan ED, Iseman MD: Multidrug-resistant and extensively drug-resistant tuberculosis: a review. Curr. Opin. Infect. Dis. 21(6), 587-595 (2008).
11. Jain A, Mondal R: Extensively drug-resistant tuberculosis: current challenges and threats. FEMS Immunol. Med. Microbiol. 53(2), 145-150 (2008).
12. Zignol M, Hosseini MS, Wright A, Weezenbak GL, Nunn P, Watt CJ: Global incidence of multidrug-resistant tuberculosis. J. Infect. Dis. 194(4), 479-485 (2006).
13. Jassal M, Bishai WR: Extensively drug-resistant tuberculosis. Lancet Infect. Dis. 9(1), 19-30 (2009).
14. LoBue P: Extensively drug-resistant tuberculosis. Curr. Opin. Infect. Dis. 22(2), 167-173 (2009).
15. Thierry D, Brisson-Noël A, Vincent-Lévy-Frébault V, Nguyen S, Guesdon JL, Gicquel B: Characterization of a Mycobacterium tuberculosis insertion sequence, IS6110, and its application in diagnosis. J. Clin. Microbiol. 28(12), 2668-2673 (1990).
16. Kamerbeek J, Schouls L, Kolk A et al.: Simultaneous detection and strain differentiation of Mycobacterium tuberculosis for diagnosis and epidemiology. J. Clin. Microbiol. 35(4), 907-914 (1997).
17. Kremer K, van Sootingen D, Frothingham R et al.: Comparison of methods based on different molecular epidemiological markers for typing of Mycobacterium tuberculosis complex strains: interlaboratory study of discriminatory power and reproducibility. J. Clin. Microbiol. 37(8), 2607-2618 (1999).
18. Kristjansson M, Green P, Manning HL et al.: Molecular confirmation of bacillus Calmette-Guerin as the cause of pulmonary infection following urinary tract, instillation. Clin. Infect. Dis. 17(2), 228-230 (1993).
19. Gegia M, Mdivani N, Mendes RE et al.: Prevalence of and molecular basis for tuberculosis drug resistance in the Republic of Georgia: validation of a QIAplex system for detection of drug resistance-related mutations. Antimicrob. Agents Chemother. 52(2), 725-729 (2008).
20. Han J, Swan DC, Smith SJ et al.: Simultaneous amplification and identification of 25 human papillomavirus types with Templex technology. J. Clin. Microbiol. 44(11), 4157-4162 (2006).
21. Phyu S, Stavrum R, Lwin T, Svendsen S, Ti T, Grewal HM: Predominance of Mycobacterium tuberculosis EAI and Beijing lineages in Yangon, Myanmar. J. Clin. Microbiol. 47(2), 335-344 (2009).
22. Tafaj S, Zhang J, Hauck Y et al.: A first insight on the genetic diversity of Mycobacterium tuberculosis complex in Albania by multi-locus variable number of tandem repeat analysis (MLVA) and spoligotyping reveals the presence of Beijing multi-drug resistant isolates. J. Clin. Microbiol. (2009).
23. Dye C: Doomsday postponed? Preventing and reversing epidemics of drug-resistant tuberculosis. Nat. Rev. Microbiol. 7(1), 81-87 (2009).
24. Ducati RG, Ruffino-Netto A, Basso LA, Santos DS: The resumption of consumption - a review on tuberculosis. Mem. Inst. Oswaldo Cruz 101(7), 697-714 (2006).
25. Gillespie SH: Tuberculosis: evolution in millennia and minutes. Biochem. Soc. Trans. 35(Pt 5), 1317-1320 (2007).
26. Böttger EC, Springer B: Tuberculosis: drug resistance, fitness, and strategies for global control. Eur. J. Pediatr. 167(2), 141-148 (2008).
27. Jarlier V, Nikaido H: Mycobacterial cell wall: structure and role in natural resistance to antibiotics. FEMS Microbiol. Lett. 123(1-2), 11-18 (1994).
28. De Rossi E, Aínsa JA, Riccardi G: Role of mycobacterial efflux transporters in drug resistance: an unresolved question. FEMS Microbiol. Rev. 30(1), 36-52 (2006).
29. Zhang Y, Heym B, Allen B, Young D, Cole ST: The catalase-peroxidase gene and isoniazid resistance of Mycobacterium tuberculosis. Nature 358(6387), 591-593 (1992).
30. Banerjee A, Dubnau E, Quemard A et al.: inhA, a gene encoding a target for isoniazid and ethionamide in Mycobacterium tuberculosis. Science 263(5144), 227-230 (1994).
31. Dessen A, Quémard A, Blanchard JS, Jacobs WR Jr, Sacchettini JC: Crystal structure and function of the isoniazid target of Mycobacterium tuberculosis. Science 267(5204), 1638-1641 (1995).
32. Rozwarski DA, Grant GA, Barton DH, Jacobs WR Jr, Sacchettini JC: Modification of the NADH of the isoniazid target (InhA) from Mycobacterium tuberculosis. Science 279(5347), 98-102 (1998).
33. Vilchèze C, Jacobs WR Jr: The mechanism of isoniazid killing: clarity through the scope of genetics. Annu. Rev. Microbiol. 61, 35-50 (2007).
34. Mdluli K, Shydea RA, Zhu Y et al.: Inhibition of a Mycobacterium tuberculosis β-ketoacyl ACP synthase by isoniazid. Science 280(5369), 1607-1610 (1998).
35. Argyrou A, Vetting MW, Aladegbami B, Blanchard JS: Mycobacterium tuberculosis dihydrofolate reductase is a target for isoniazid. Nat. Struct. Mol. Biol. 13(5), 408-413 (2006).
36. Shi R, Itagaki N, Sugawara I: Overview of anti-tuberculosis (TB) drugs and their resistance mechanisms. Mini Rev. Med. Chem. 7(11), 1177-1185 (2007).
37. Slayden RA, Barry CE 3rd: The genetics and biochemistry of isoniazid resistance in Mycobacterium tuberculosis. Microbes Infect. 2(6), 659-669 (2000).
38. Lee AS, Teo AS, Wong SY: Novel mutations in ndh in isoniazid-resistant Mycobacterium tuberculosis isolates. Antimicrob. Agents Chemother. 45(7), 2157-2159 (2001).
39. + ratio mediates coresistance to isoniazid and ethionamide in mycobacteria. Antimicrob. Agents Chemother. 49(2), 708-720 (2005).
40. DeBarber AE, Mdluili K, Bosman M, Bekker L, Barry CE 3rd: Ethionamide activation and sensitivity in multi-drug resistant Mycobacterium tuberculosis. Proc. Natl Acad. Sci. USA 97(17), 9677-9682 (2000).
41. Wang F, Langley R, Gulten G et al.: Mechanism of thioamide drug action against tuberculosis and leprosy. J. Exp. Med. 204(1), 73-78 (2007).
42. Morlock GP, Metchcock B, Sikes D, Crawford JT, Cooksey RC: EthA, inhA, and katG loci of ethionamide-resistant clinical Mycobacterium tuberculosis isolates. Antimicrob. Agents Chemother. 47(12), 3799-3805 (2003).
43. Vilchèze C, Wang F, Arai M et al.: Transfer of a point mutation in Mycobacterium tuberculosis inhA resolves the target of isoniazid. Nat. Med. 12(9), 1027-1029 (2006).
44. Subba Rao G, Vijayakrishnan R, Kumar M: Structure-based design of a novel class of potent inhibitors of InhA, the enoyl acyl carrier protein reductase from Mycobacterium tuberculosis: a computer modelling approach. Chem. Biol. Drug Des. 72(5), 444-449 (2008).
45. Baulard AR, Betts JC, Engohang-Ndong J et al.: Activation of the pro-drug ethionamide is regulated in mycobacteria. J. Biol. Chem. 275(36), 28326-28331 (2000).
46. Hollinrake K: Acute hepatic necrosis associated with ethionamide. Br. J. Dis. Chest 62(3), 151-154 (1968).
47. Weber W, Schoenmakers R, Keller B et al.: A synthetic mammalian gene circuit reveals antituberculosis compounds. Proc. Natl Acad. Sci. USA. 105(29), 9994-9998 (2008).
48. Engohang-Ndong J, Baillat D, Aumercier M et al.: EthR, a repressor of the TetR/CamR family implicated in ethionamide resistance in mycobacteria, octamerizes cooperatively on its operator. Mol. Microbiol. 51(1), 175-188 (2004).
49. Dover LG, Alahari A, Gratraud P et al.: EthA, a common activator of thiocarbamide-containing drugs acting on different mycobacterial targets. Antimicrob. Agents Chemother. 51(3), 1055-1063 (2007).
50. Alahari A, Alibaud L, Trivelli X et al.: Mycolic acid methyltransferase, MmaA4, is necessary for thiacetazone susceptibility in Mycobacterium tuberculosis. Mol. Microbiol. 71(5), 1263-1277 (2009).
51. Vilchèze C, Av-Gay Y, Attarian R et al.: Mycothiol biosynthesis is essential for ethionamide susceptibility in Mycobacterium tuberculosis. Mol Microbiol. 69(5), 1316-1329 (2008).
52. Wolucka BA: Biosynthesis of D-arabinose in mycobacteria - a novel bacterial pathway with implications for antimycobacterial therapy. FEBS J. 275(11), 2691-2711 (2008).
53. Telenti A, Philip WJ, Sreevatsan S et al.: The emb operon, a gene cluster of Mycobacterium tuberculosis involved in resistance to ethembutol. Nat. Med. 3(5), 567-570 (1997).
54. Srivastava S, Garg A, Ayyagari A, Nyati KK, Dhole TN, Dwivedi SK: Nucleotide polymorphism associated with ethambutol resistance in clinical isolates of Mycobacterium tuberculosis. Curr. Microbiol. 53(5), 401-405 (2006).
55. Safi H, Sayers B, Hazbón MH, Alland D: Transfer embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin. Antimicrob. Agents Chemother. 52(6), 2027-2034 (2008).
56. Ramaswamy S, Amin AG, Koksel S et al.: Molecular genetic analysis of nucleotide polymorphisms associated with ethambutol resistance in human isolates of Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 44(2), 326-336 (2000).
57. Alland D, Kramnik I, Weisbrod TR et al.: Identification of differentially expressed mRNA in prokaryotic organisms by customized amplification libraries (DECAL): the effect of isoniazid on gene expression in Mycobacterium tuberculosis. Proc. Natl Acad. Sci USA 95(22), 13227-13232 (1998).
58. Hazbón MH, Motiwala AS, Cavatore M, Brimacombe M, Whittam TS, Alland D: Convergent evolutionary analysis identifies significant mutations in drug resistance targets of Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 52(9), 3369-3376 (2008).
59. Lambert MP, Neuhaus FC: Mechanism of D-cycloserine action: alanine racemase from Escherichia coli W. J. Bacteriol. 110(3), 978-987 (1972).
60. David HL, Takayama K, Goldman DS: Susceptibility of mycobacterial D-alanyl-D-alanine synthetase to [s D s]-cycloserine. Am. Rev. Respir. Dis. 100(4), 579-581 (1969).
61. Strych U, Penland RL, Jimenez M, Krause KL, Benedik MJ: Characterization of the alanine racemases from two mycobacteria. FEMS Microbiol. Lett. 196(2), 93-98 (2001).
62. Cáceres NE, Harris NB, Wellehan JF, Feng Z, Kapur V, Barletta RG: Overexpression of the D-alanine racemase gene confers resistance to D-cycloserine in Mycobacterium smegmatis. J. Bacteriol. 179(16), 5046-5055 (1997).
63. Feng Z, Barletta RG: Roles of Mycobacterium. smegmatis D-alanine:D-alanine ligase and D-alanine racemase in the mechanisms of action and of resistance to the peptidoglycan inhibitor D-cycloserine. Antimicrob. Agents Chemother. 47(1), 283-291 (2003).
64. Zhang Y: The magic bullets and tuberculosis drug targets. Annu. Rev. Pharmacol. Toxicol. 45, 529-564 (2005).
65. Campbell EA, Korzheva N, Mustaev A et al.: Structural mechanism for rifampicin inhibition of bacterial RNA polymerase. Cell 104(6), 901-912 (2001).
66. Telenti A, Imboden P, Marchesi F et al.: Detection of rifampicin-resistance mutations in Mycobacterium tuberculosis. Lancet 341(8846), 647-650 (1993).
67. Siddiqi N, Das R, Pathak N et al.: Mycobacterium tuberculosis isolate with a distinct genomic identity overexpresses a tap-like efflux pump. Infection 32(2), 109-111 (2004).
68. Jiang X, Zhang W, Zhang Y et al.: Assessment of efflux pump gene expression in a clinical isolate Mycobacterium tuberculosis by real-time reverse transcription PCR. Microb. Drug Resist. 14(1), 7-11 (2008).
69. Moadebi S, Harder CK, Fitzgerald MJ, Elwood KR, Marra F: Fluoroquinolones for the treatment of pulmonary tuberculosis. Drugs 67(14), 2077-2099 (2007).
70. Ginsburg AS, Grosser JH, Bishai WR: Fluoroquinolones, tuberculosis, and resistance. Lancet Infect. Dis. 3(7), 432-442 (2003).
71. Takiff HE, Salazar L, Guerrero C et al.: Cloning and nucleotide sequence of Mycobacterium tuberculosis gyrA and gyrB genes and detection of quinolone resistance mutations. Antimicrob. Agents Chemother. 38(4), 773-780 (1994).
72. Wang JY, Lee LN, Lai HC et al.: Fluoroquinolone resistance in Mycobacterium tuberculosis isolates: associated genetic mutations and relationship to antimicrobial exposure. J. Antimicrob. Chemother. 59(5), 860-865 (2007).
73. Matrat S, Aubry A, Mayer C, Jarlier V, Cambau E: Mutagenesis in the α3α4 GyrA helix and in the toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones. Antimicrob. Agents Chemother. 52(8), 2909-2914 (2008).
74. Agrawal D, Udwadia ZF, Rodriguez C, Mehta A: Increasing incidence fluoroquinolone-resistant Mycobacterium tuberculosis in Mumbai, India. Int. J. Tuberc. Lung Dis. 13(1), 79-83 (2009).
75. Spotts CR, Stanier RY: Mechanism of streptomycin action on bacteria: a unitary hypothesis. Nature 192, 633-637 (1961).
76. Davies J, Gorini L, Davis BD: Misreading of RNA codewords induced by aminoglycoside antibiotics. Mol. Pharmacol. 1(1), 93-106 (1965).
77. Honoré N, Cole ST: Streptomycin resistance in mycobacteria. Antimicrob. Agents Chemother. 38(2), 238-242 (1994).
78. Brink MF, Verbeet MP, de Boer HA: Formation of the central pseudoknot in 16S rRNA is essential for initiation of translation. EMBO J. 12(10), 3987-3996 (1993).
79. Vila-Sanjurjo A, Lu Y, Aragonez JL, Starkweather RE, Sasikumar M, O'Connor M: Modulation of 16S rRNA function by ribosomal protein S12 Biochim. Biophys. Acta 1769(7-8), 462-467 (2007).
80. Okamoto S, Tamaru A, Nakajima C et al.: Loss of a conserved 7-methylguanosine modification in 16S rRNA confers low-level streptomycin resistance in bacteria. Mol. Microbiol. 63(4), 1096-1106 (2007).
81. Spies FS, da Silva PE, Ribeiro MO, Rossetti ML, Zaha A: Identification of mutations related to streptomycin resistance in clinical isolates of Mycobacterium tuberculosis and possible involvement of efflux mechanism. Antimicrob. Agents Chemother. 52(8), 2947-2949 (2008).
82. Danilchanka O, Mailaender C, Niederweis M: Identification of a novel multidrug efflux pump of Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 52(7), 2503-2511 (2008).
83. Richter E, Rüsch-Gerdes S, Hillemann D: First linezolid-resistant clinical isolates of Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 51(4), 1534-1536 (2007).
84. Hillemann D, Rüsch-Gerdes S, Richter E: In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants. Antimicrob. Agents Chemother. 52(2), 800-801 (2008).
85. Zhang Y, Mitchison D: The curious characteristics of pyrazinamide: a review. Int. J. Tuberc. Lung Dis. 7(1), 6-21 (2003).
86. Zimhony O, Vilchèze C, Arai M, Welch JT, Jacobs WR Jr: Pyrazinoic acid and its n-propyl ester inhibit fatty acid synthase type I in replicating tubercle bacilli. Antimicrob. Agents Chemother. 51(2), 752-754 (2007).
87. Singh P, Mishra AK, Malonia SK et al.: The paradox of pyrazinamide: an update on the molecular mechanisms of pyrazinamide resisrance in mycobacteria. J. Commun. Dis. 38(3), 288-298 (2006).
88. Juréen P, Werngren J, Toro JC, Hoffner S: Pyrazinamide resistance and pncA gene mutations in Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 52(5), 1852-1854 (2008).
89. Cole ST, Brosch R, Parkhill J et al.: Deciphering the biology of Mycobacterium tuberculosis from the complete genome sequence. Nature 393(6685), 537-544 (1998).
90. Andries K, Verhasselt P, Guillemont J et al.: A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science 307(5707), 223-227 (2006).
91. Williams KJ, Duncan K: Current strategies for identifying and validating targets for new treatment-shortening drugs for TB. Curr. Mol. Med. 7(3), 297-307 (2007).
92. Murillo AC, Li HY, Alber T et al.: High throughput crystallography of TB drug targets. Infect. Disord. Drug Targets 7(2), 127-139 (2007).
93. Lamichhane G, Tyagi S, Bishai WR: Designer arrays for defined mutant analysis to detect genes essential for survival of Mycobacterium tuberculosis in mouse lungs. Infect. Immun. 73(4), 2533-2540 (2005).
94. Sassetti CM, Boyd DH, Rubin EJ: Genes required for mycobacterial growth defined by high density mutagenesis. Mol. Microbiol. 48(1), 77-84 (2003).
95. Sassetti CM, Rubin EJ: Genetic requirements for mycobacterial survival during infection. Proc. Natl Acad. Sci. USA 100(22), 12989-12994 (2003).
96. Stirrett KL, Ferreras JA, Jayaprakash V, Sinha BN, Ren T, Quadri LE: Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis. Bioorg. Med. Chem. Lett. 18(8), 2662-2668 (2008).
97. Bhave DP, Muse WB 3rd, Carroll KS: Drug targets in mycobacterial sulfur metabolism. Infect. Disord. Drug Targets. 7(2), 140-158 (2007).
98. Vicente M, Hodgson J, Massidda O, Tonjum T, Henriques-Normark B, Ron EZ: The fallacies of hope: will we discover new antibiotics to combat pathogenic bacteria in time? FEMS Microbiol. Rev. 30(6), 841-852 (2006).
99. Vohra R, Gupta M, Chaturvedi R, Singh Y: Attack on the scourge of tuberculosis: patented drug targets. Recent Pat. Antiinfect. Drug Discov. 1(1), 95-106 (2006).
100. Ginsberg AM: Emerging drugs for active tuberculosis. Semin. Respir. Crit. Care Med. 29(5), 552-559 (2008).
101. Lenaerts AJ, Degroote MA, Orme IM: Preclinical testing of new drugs for tuberculosis: current challenges. Trends Microbiol. 16(2), 48-54 (2008).
102. Rivers EC, Mancera RL: New anti-tuberculosis drugs with novel mechanisms of action. Curr. Med. Chem. 15(19), 1956-1967 (2008).
103. Burman WJ, Goldberg S, Johnson JL et al.: Moxifloxacin versus ethambutol in the first 2 months of treatment for pulmonary tuberculosis. Am. J. Respir. Crit. Care Med. 174(3), 331-338 (2006).
104. Rustomjee R, Lienhardt C, Kanyok T et al.: A Phase II study of the sterilising activities of ofloxacin, gatifloxacin and moxifloxacin in pulmonary tuberculosis. Int. J. Tuberc. Lung Dis. 12(2), 128-138 (2008).
105. Koul A, Dendouga N, Vergauwen K et al.: Diarylquinolines target subunit c of mycobacterial ATP synthase. Nat. Chem. Biol. 3(6), 323-324 (2007).
106. Rao SP, Alonso S, Rand L, Dick T, Pethe K: The protonmotive force is required for maintaining ATP homeostasis and viability of hypoxic, nonreplicating Mycobacterium tuberculosis. Proc. Natl Acad. Sci. USA 105(33), 11945-11950 (2008).
107. Tomioka H: Current status of some antituberculosis drugs and the development of new antituberculous agents with special reference to their in vitro and in vivo antimicrobial activities. Curr. Pharm. Des. 12(31), 4047-4070 (2006).
108. Haagsma AC, Ibrahim RA, Wagner MJ et al.: Selectivity of TMC207 towards mycobacterial ATP synthase as compared with the eukaryotic homologue. Antimicrob. Agents Chemother. 53(3), 1290-1292 (2009).
109. Stover CK, Warrener P, VanDevanter DR. et al.: A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature 405(6789), 962-966 (2000).
110. Singh R, Manjunatha U, Boshoff HI et al.: PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. Science 322(5906), 1392-1395 (2008).
111. Manjunatha UH, Lahiri R, Randhawa B, Dowd CS, Krahenbuhl JU, Barry CE 3rd: Mycobacterium leprae is naturally resistant to PA-824. Antimicrob. Agents Chemother. 50(10), 3350-3354 (2006).
112. Tyagi S, Nuermberger E, Yoshimatsu T et al.: Bactericidal activity of the nitroimidazopyran PA-824 in a murine model of tuberculosis. Antimicrob. Agents Chemother. 49(6), 2289-2293 (2005).
113. Lenaerts AJ, Gruppo V, Marietta KS et al.: Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob. Agents Chemother. 49(6), 2294-2301 (2005).
114. Nuermberger E, Rosenthal I, Tyagi S et al.: Combination chemotherapy with the nitroimidazopyran PA-824 and first-line drugs in a murine model of tuberculosis. Antimicrob. Agents Chemother. 50(8), 2621-2625 (2006).
115. Matsumoto M, Hashizume H, Tomishige T. et al.: OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice. PLoS Med. 3(11), e466 (2006).
116. Deidda D, Lampis G, Fioravanti R et al.: Bactericidal activities of the pyrrole derivative BM212 against multidrug-resistant and intramacrophagic Mycobacterium tuberculosis strains. Antimicrob. Agents Chemother. 42(11), 3035-3037 (1998).
117. Biava M: BM212 and its derivatives as a new class of antimycobacterial active agents. Curr. Med. Chem. 9(21), 1859-1869 (2002).
118. Biava M, Porretta GC, Manetti F: New derivatives of BM212: a class of antimycobacterial compounds based on the pyrrole ring as a scaffold. Mini Rev. Med. Chem. 7(1), 65-78 (2007).
119. Protopopova M, Hanrahan C, Nikonenko B et al.: Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines. J. Antimicrob. Chemother. 56(5), 968-974 (2005).
120. Chen P, Gearhart J, Protopopova M, EinckL, Nacy CA: Synergistic interactions of SQ109, a new ethylene diamine, with front-line antitubercular drugs in vitro. J. Antimicrob. Chemother. 58(2), 332-337 (2006).
121. Madariaga MG, Lalloo UG, Swindells S: Extensively drug-resistant tuberculosis. Am. J. Med. 121(10), 835-844 (2008).
122. Showalter HD, Denny WA: A roadmap for drug discovery and its translation to small molecule agents in clinical development for tuberculosis treatment. Tuberculosis (Edinb.) 88(Suppl. 1), S3-S17 (2008).
123. Tomioka H, Namba K: Development of antituberculous drugs: current status and future prospects. Kekkaku 81(12), 753-774 (2006).
124. Makarov V, Manina G, Mikusova K et al.: Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science DOI:10.1126/.science.1171583 (2009).