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88. Zhang Y, Wade MM, Scorpio A, Zhang H, Sun Z (2003) Mode of action of pyrazinamide:
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89. Boshoff HI, Mizrahi V, Barry CE (2002) Effects of pyrazinamide on fatty acid synthesis by
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90. Mdluli K, Ma Z (2007) Mycobacterium tuberculosis DNA gyrase as a target for drug
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91. Onodera Y, Tanaka M, Sato K (2001) Inhibitory activity of quinolones against DNA gyrase
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92. Blondeau JM (2004) Fluoroquinolones: mechanism of action, classification, and development of resistance. Surv Ophthalmol 49:S73–S78
93. Piton J, Petrella S, Delarue M, André-Leroux G, Jarlier V, Aubry A, Mayer C (2010)
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of DNA gyrase B inhibitors. Fut Med Chem 10:1207–1227
95. Chopra S, Matsuyama K, Tran T, Malerich JP, Wan B, Franzblau SG, Lun S, Guo H,
Maiga MC, Bishai WR (2011) Evaluation of gyrase B as a drug target in Mycobacterium
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96. Shirude PS, Madhavapeddi P, Tucker JA, Murugan K, Patil V, Basavarajappa H,
Raichurkar AV, Humnabadkar V, Hussein S, Sharma S, Ramya VK, Narayan CB,
Balganesh TS, Sambandamurthy VK (2013) Aminopyrazinamides: novel and specific GyrB
inhibitors that kill replicating and nonreplicating Mycobacterium tuberculosis. ACS Chem
Biol 8:519–523
97. Pedgaonkar GS, Sridevi JP, Jeankumar VU, Saxena S, Devi PB, Renuka J, Yogeeswari P,
Sriram D (2014) Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors
of Mycobacterium tuberculosis InhA. Bioorg Med Chem 22:6134–6145
98. Reddy KI, Srihari K, Renuka J, Sree KS, Chuppala A, Jeankumar VU, Sridevi JP, Babu KS,
Yogeeswari P, Sriram D (2014) An efficient synthesis and biological screening of
benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB
inhibition. Bioorg Med Chem 22:6552–6563
99. Renuka J, Reddy KI, Srihari K, Jeankumar VU, Shravan M, Sridevi JP, Yogeeswari P,
Babu KS, Sriram D (2014) Design, synthesis, biological evaluation of substituted
benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis. Bioorg Med
Chem 22:4924–4934
100. Davis CK, Nasla K, Anjana A, Rajanikant G (2018) Taxifolin as dual inhibitor of Mtb DNA
gyrase and isoleucyl-tRNA synthetase: in silico molecular docking, dynamics simulation and
in vitro assays. Silico Pharmacol 6:8
342
A. C. Pushkaran et al.
synthetase as a novel antibiotic strategy against tuberculosis: demonstration of efficacy
in vivo. Infect Immun 71:456–464
84. Kasbekar M, Fischer G, Mott BT, Yasgar A, Hyvönen M, Boshoff HI, Abell C, Barry CE,
Thomas CJ (2016) Selective small molecule inhibitor of the Mycobacterium tuberculosis
fumarate hydratase reveals an allosteric regulatory site. Proc Natl Acad Sci 113:7503–7508
85. Li M, Huang Y-J, Tai PC, Wang B (2008) Discovery of the first SecA inhibitors using
structure-based virtual screening. Biochem Biophys Res Commun 368:839–845
86. Chen W, Huang Y-J, Gundala SR, Yang H, Li M, Tai PC, Wang B (2010) The first low lM
SecA inhibitors. Bioorg Med Chem 18:1617–1625
87. Via LE, Savic R, Weiner DM, Zimmerman MD, Prideaux B, Irwin SM, Lyon E, O’Brien P,
Gopal P, Eum S (2015) Host-mediated bioactivation of pyrazinamide: implications for
efficacy, resistance, and therapeutic alternatives. ACS Infect Dis 1:203–214
88. Zhang Y, Wade MM, Scorpio A, Zhang H, Sun Z (2003) Mode of action of pyrazinamide:
disruption of Mycobacterium tuberculosis membrane transport and energetics by pyrazinoic
acid. J Antimicrob Chemother 52:790–795
89. Boshoff HI, Mizrahi V, Barry CE (2002) Effects of pyrazinamide on fatty acid synthesis by
whole mycobacterial cells and purified fatty acid synthase I. J Bacteriol 184:2167–2172
90. Mdluli K, Ma Z (2007) Mycobacterium tuberculosis DNA gyrase as a target for drug
discovery. Infect Disorders-Drug Targets (Form Curr Drug Targets-Infect Disorders) 7:159–
168
91. Onodera Y, Tanaka M, Sato K (2001) Inhibitory activity of quinolones against DNA gyrase
of Mycobacterium tuberculosis. J Antimicrob Chemother 47:447–450
92. Blondeau JM (2004) Fluoroquinolones: mechanism of action, classification, and development of resistance. Surv Ophthalmol 49:S73–S78
93. Piton J, Petrella S, Delarue M, André-Leroux G, Jarlier V, Aubry A, Mayer C (2010)
Structural insights into the quinolone resistance mechanism of Mycobacterium tuberculosis
DNA gyrase. PLoS ONE 5:e12245
94. Barancokova M, Kikelj D, Ilas J (2018) Recent progress in the discovery and development
of DNA gyrase B inhibitors. Fut Med Chem 10:1207–1227
95. Chopra S, Matsuyama K, Tran T, Malerich JP, Wan B, Franzblau SG, Lun S, Guo H,
Maiga MC, Bishai WR (2011) Evaluation of gyrase B as a drug target in Mycobacterium
tuberculosis. J Antimicrob Chemother 67:415–421
96. Shirude PS, Madhavapeddi P, Tucker JA, Murugan K, Patil V, Basavarajappa H,
Raichurkar AV, Humnabadkar V, Hussein S, Sharma S, Ramya VK, Narayan CB,
Balganesh TS, Sambandamurthy VK (2013) Aminopyrazinamides: novel and specific GyrB
inhibitors that kill replicating and nonreplicating Mycobacterium tuberculosis. ACS Chem
Biol 8:519–523
97. Pedgaonkar GS, Sridevi JP, Jeankumar VU, Saxena S, Devi PB, Renuka J, Yogeeswari P,
Sriram D (2014) Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors
of Mycobacterium tuberculosis InhA. Bioorg Med Chem 22:6134–6145
98. Reddy KI, Srihari K, Renuka J, Sree KS, Chuppala A, Jeankumar VU, Sridevi JP, Babu KS,
Yogeeswari P, Sriram D (2014) An efficient synthesis and biological screening of
benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB
inhibition. Bioorg Med Chem 22:6552–6563
99. Renuka J, Reddy KI, Srihari K, Jeankumar VU, Shravan M, Sridevi JP, Yogeeswari P,
Babu KS, Sriram D (2014) Design, synthesis, biological evaluation of substituted
benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis. Bioorg Med
Chem 22:4924–4934
100. Davis CK, Nasla K, Anjana A, Rajanikant G (2018) Taxifolin as dual inhibitor of Mtb DNA
gyrase and isoleucyl-tRNA synthetase: in silico molecular docking, dynamics simulation and
in vitro assays. Silico Pharmacol 6:8
342
A. C. Pushkaran et al.