Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids

Quinoline and quinolones: promising scaffolds for future antimycobacterial agents

“…The authors suggested that the presence of electron-donating -CH 3 group stabilize the pyrazole ring and thus make the 46a more active against M. tuberculosis Substitution pattern at C-7 demonstrated the following order of activity: fused piperazines and piperidines4(thio) morpholines4substituted piperazines4substituted piperidines. It was suggested that the introduction of bulky lipophilic secondary amines at C-7 position improved antimycobacterial activity due to more penetration of these compounds into mycobacterial cells 35 . In continuation, Senthilkumar et al also reported novel fluoroquinolones by varying the substitution at N-1 and C-7 positions (47).…”

2D-QSAR analysis on some 8-methoxy quinoline derivatives as H37RV (MTB) inhibitors with comparison of different model

“…8-methoxyquinoline carboxylic acids exhibiting the potent antimycobacterial Activity was taken from the reported work by Palaniappan Senthilkumar et al 11 .…”

Role of quinolones and quinoxaline derivatives in the advancement of treatment of tuberculosis

“…Compound (16) exhibited MIC99 of 0.19 μM and 0.09 μM against MTB and MDR-TB, respectively and decreased the bacterial load in lung and spleen tissues with 1.91 and 2.91-log10 protections, respectively, in the in vivo animal model at a dose of 50 mg/kg body weight [105][106][107]. Compound (17) decreased the bacterial load in lung and spleen tissues with 2.54 and 2.92-log10 protections [111], while (18) decreased the bacterial load by 30% and 42%, respectively, at a dose of 50 mg/kg body weight [105][106][107]. In an effort to increase the antitubercular potency of quinolones, 1-(cyclopropyl/2,4-difluorophenyl/tert-butyl)-1,4-dihydro-8-methyl-6-nitro-4-oxo-7-(substitutedsecondary-amino)quinoline-3-carboxylic acids.…”