Ring-substituted quinolines as potential anti-tuberculosis agents Original Research Article

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 μg/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: ⩽6.25 μg/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 μg/mL.