Ring-substituted quinolines as potential anti-tuberculosis agents.
We report in vitro antimycobacterial properties of ring-substituted quinolines (series 1-4) constituting 56 analogues against drug-sensitive and drug-resistant M. tuberculosis H37Rv strains. The most effective compounds 2h (R1 = R2 = c-C6H11, R3 = NO2, series 1) and 13g (R1 = OC7H15, R2 = NO2, series 4) have exhibited an MIC value of 1 microg/mL against drug-sensitive M. tuberculosis H37Rv strain that is comparable to first line anti-tuberculosis drug, isoniazid. Selected analogues (2d, 2g, 2h, 4e, 6b, 13b, 13g, and 14e, MIC: < or = 6.25 microg/mL) upon further evaluation against single-drug-resistant (SDR) strains of M. tuberculosis H37Rv have produced potent efficacy in the range between 6.25 and 50 microg/mL.
Vangapandu
Suryanarayana
S
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
Jain
Meenakshi
M
Jain
Rahul
R
Kaur
Sukhraj
S
Singh
Prati Pal
PP
D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014376:Tuberculosis / Q000188:drug therapy; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy
D000995:Antitubercular Agents; D011804:Quinolines