Bending the curve - ending TB: Annual report 2017 India:
World Health Organization, Regional Office for South-East
Asia; 2017. Licence: CC BY-NC-SA 3.0 IGO.
Gill C, Jadhav G, Mohammad Shaikh M, et al. Clubbed [1,2,3] triazoles by fluorine benzimidazole: A novel approach to H37Rv inhibitors as a potential treatment for tuberculosis. Bioorg Med Chem Lett 2008; 18: 6244-7.
Purser S, Moore PR, Swallow S, Gouverneur V. Fluorine in medicinal chemistry. Chem Soc Rev 2008; 37(2): 320-30.
Kirk KL. Fluorine in medicinal chemistry: Recent therapeutic applications of fluorinated small molecules. J Fluor Chem 2006; 127: 1013-29.
Landelle G, Panossian A, Leroux FR. Trifluoromethyl ethers and -thioethers as tools for medicinal chemistry and drug discovery. Curr Top Med Chem 2014; 14(7): 941-51.
Maccari R, Ottana R, Vigorita MG. In vitro advanced antimycobacterial screening of isoniazid-related hydrazones, hydrazides and cyanoboranes: part 14. Bioorg Med Chem Lett 2005; 15: 2509-13.
Frédéric RL, Manteau B, Vors JP, Pazenok S. Trifluoromethyl ethers - synthesis and properties of an unusual substituent. Beilstein J Org Chem 2008; 4(13): 1-15.
Kovacevic B, Maksić ZB, Primorac M. Acidity of substituted benzenes - an ab initio study of the influence of methoxy, trifluoromethyl and trifluoromethoxy groups by a novel trichotomy formula. Eur J Org Chem 2003; 19: 3777-83.
Wermuth CG. The Practice of Medicinal Chemistry. 3rd ed. Academic Press: New York 2015.
Banks RE, Smart BE, Tatlow JC. Organofluorine Chemistry Principles and Commercial Applications. 3rd Eds. Plenum
Press: New York 1994.
Muller K, Faeh C, Diederich F. Fluorine in pharmaceuticals: looking beyond intuition. Science 2007; 317: 1881-6.
Smart BE. Fluorine substituent effects on bioactivity. J Fluor Chem 2001; 109(1): 3-11.
Bégué JP, Delpon DB. Bioorganic and medicinal chemistry of fluorine. 1st Eds. . Wiley & Sons: New York 2008.
Castagnetti E, Schlosser M. The trifluoromethoxy group: a long-range electron-withdrawing substituent. Chem A Eur J 2002; 8(4): 799-04.
Diacon AH, Dawson R, Hanekom M, et al. Early bactericidal activity and pharmacokinetics of PA824 in smear positive tuberculosis patients. Antimicrob Agents Chemother 2010; 54(8): 3402-7.
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 2006; 3: 2131-43.
Hoagland DT, Liu J, Lee RB, Lee RE. New agents for the treatment of drug-resistant Mycobacterium tuberculosis. Adv Drug Deliv Rev 2016; 102: 55-72.
Upton AM, Cho S, Yang TJ, et al. In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis. Antimicrob Agents Chemother 2015; 59(1): 13644.
Pethe K, Bifani P, Jang J, et al. Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. Nat Med 2013; 19: 1157-60.
Arora SK, Anuradha K, Avhad AJ. Phase 1 clinical trial of LL-3858 (Sudoterb), a potential candidate for the treatment of MDR tuberculosis. Int J Tuberc Lung Dis 2008; 12: S319.
Adhvaryu M, Vakharia B. Drug-resistant tuberculosis: emerging treatment Options. Clin Pharmacol 2011; 3: 51-67.
Makarov V, Manina G, Mikusova K, et al. Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. Science 2009; 324(5928): 801-4.
Pasca MR, Degiacomi G, Ribeiro AL, et al. Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones. Antimicrob Agents Chemother 2010; 54(4): 1616-8.
Bermudez LE, Kolonoski P, Wu M, Aralar PA, Inderlied CB, Young LS. Mefloquine is active in vitro and in vivo against Mycobacterium avium complex. Antimicrob Agents Chemother 1999; 43: 1870-4.
Nannini EC, Keating M, Binstock P, Samonis G, Kontoyiannis DP. Successful treatment of refractory disseminated Mycobacterium avium complex infection with the addition of linezolid and mefloquine. J Infect 2002; 44(3): 201-3.
Mao J, Yuan H, Wang Y, et al. Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs. Synthesis and anti-tuberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs. Bioorg Med Chem Lett 2010; 20(3): 1263-8.
Lilienkampf A, Mao J, Wan B, Wang Y, Franzblau SG, Kozikowski AP. Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis. J Med Chem 2009; 52(7): 2109-18.
Mital A, Negi VS, Ramachandran U. Synthesis and antimycobacterial activities of certain trifluoromethyl-amino quinoline derivatives. Arkivoc 2006; 10: 220-7.
Eswaran S, Adhikari AV, Kumar R. New 1,3-oxazolo[4,5-c]quinoline derivatives: synthesis and evaluation of antibacterial and antituberculosis properties. Eur J Med Chem 2010; 45(3): 957-66.
Eswaran S, Adhikari AV, Pal NK, et al. Targeting tuberculosis and malaria through inhibition of enoyl reductase: compound activity and structural data. J Biol Chem 2003; 278: 20851-9.
Kuo MR, Morbidoni HR, Alland D, et al. Targeting tuberculosis and malaria through inhibition of enoyl reductase: compound activity and structural data. J Biol Chem 2003; 278: 20851-9.
Almeida da Silva PE, Ramosa DF, Bonacorso HG, et al. Synthesis and in vitro antimycobacterial activity of 3-substituted 5-hydroxy-5-trifluoro[chloro]methyl-4,5 dihydro-1 H-1-(isonicotinoyl) pyrazoles. Int J Antimicrob Agents 2008; 32: 139-44.
Addla D, Jallapally A, Gurram D, Yogeeswari P, Sriram D, Kantevari S. Rational design, synthesis and antitubercular evaluation of novel 2-(trifluoromethyl) phenothiazine-[1,2,3]triazole hybrids. Bioorg Med Chem Lett 2014; 24(1): 233-6.
Abdel-Rahman HM, El-Koussi NA, Hassan HY. Fluorinated 1,2,4-Triazolo[1,5-a] pyrimidine-6-carboxylic acid derivatives as antimycobacterial agents. Arch Pharm Chem Life Sci 2009; 342(2): 94-9.
Šink R, Sosi I, Živec M, et al. Design, synthesis and evaluation of new thiadiazolebased direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis. J Med Chem 2015; 58(2): 613-24.
Yokokawa F, Wang G, Chan WL, et al. Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents. ACS Med Chem Lett 2013; 4(5): 451-5.
Onajole OK, Pieroni M, Tipparaju SK, et al. Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains. J Med Chem 2013; 56: 4093-3.
Maccari R, Ottana R, Monforte F, Vigorita MG. In vitro antimycobacterial activities of 2′-monosubstituted isonicotinohydrazides and their cyanoborane adducts. Antimicrob Agents Chemother 2002; 46(2): 294-9.
Güzel O, Karali N, Salman A. Synthesis and antituberculosis activity of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazone derivatives. Bioorg Med Chem 2008; 16: 8976-87.
Palmer BD, Thompson AM, Sutherland HS, et al. Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6s)-2-nitro-6-[4-(trifluoromethoxy) benzyl]oxy-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824). J Med Chem 2010; 53: 282-94.
Sriram D, Yogeeswari P, Dinakaran M, Thirumurugan R. Antimycobacterial activity of novel 1-(5-cyclobutyl-1,3-oxazol-2-yl)-3-(sub)phenyl/pyridylthiourea compounds endowed with high activity toward multidrug-resistant Mycobacterium tuberculosis. J Antimicrob Chemother 2007; 59: 1194-6.
Lilienkampf A, Pieroni M, Wan B, Wang Y, Franzblau SG, Kozikowski AP. Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis: a potent and selective series for further drug development. J Med Chem 2010; 53: 678-88.
Yang Y, Wang Z, Yang J, et al. Design, synthesis and evaluation of novel molecules with a diphenyl ether nucleus as potential antitubercular agents. Bioorg Med Chem Lett 2012; 22: 954-7.
Guo S, Song Y, Huang Q, et al. Identification, synthesis, and pharmacological evaluation of tetrahydroindazole based ligands as novel antituberculosis agents. J Med Chem 2010; 53: 649-59.
Dolezal M, Cmedlova P, Palek L, et al. Synthesis and antimycobacterial evaluation of substituted pyrazinecarboxamides. Eur J Med Chem 2008; 43(5): 1105-13.
Zhang D, Lu Y, Liu K, et al. Identification of less lipophilic riminophenazine derivatives for the treatment of drug-resistant tuberculosis. J Med Chem 2012; 55(19): 8409-17.
Krátký M, Vinšová J, Novotná E, et al. Salicylanilide derivatives block Mycobacterium tuberculosis through inhibition of isocitrate lyase and methionine aminopeptidase. Tuberculosis 2012; 92: 434-9.
Krátký M, Vinšová J, Novotná E, Mandíková J, Trejtnar F, Stolaříková J. Antibacterial activity of salicylanilide 4-(trifluoromethyl) benzoates. Molecules 2013; 18: 3674-88.
Sun D, Scherman MS, Jones V, et al. Discovery, synthesis, and biological evaluation of piperidinol analogs with anti-tuberculosis activity. Bioorg Med Chem 2009; 17(10): 3588-94.