| Summary: | A series of ethyl 1-(substituted benzoyl)-5-methylpyrrolo[1,2-<i>a</i>]quinoline-3-carboxylates <b>4a</b>–<b>f</b> and dimethyl 1-(substituted benzoyl)-5-methylpyrrolo[1,2-<i>a</i>]quinoline-2,3-dicarboxylates <b>4g</b>–<b>k</b> have been synthesized and evaluated for their anti-tubercular (TB) activities against H37Rv (American Type Culture Collection (ATCC) strain 25177) and multidrug-resistant (MDR) strains of <i>Mycobacterium tuberculosis</i> by resazurin microplate assay (REMA). Molecular target identification for these compounds was also carried out by a computational approach. All test compounds exhibited anti-tuberculosis (TB) activity in the range of 8–128 µg/mL against H37Rv. The test compound dimethyl-1-(4-fluorobenzoyl)-5-methylpyrrolo[1,2-<i>a</i>]quinoline-2,3-dicarboxylate <b>4j</b> emerged as the most promising anti-TB agent against H37Rv and multidrug-resistant strains of <i>Mycobacterium tuberculosis</i> at 8 and 16 µg/mL, respectively. In silico evaluation of pharmacokinetic properties indicated overall drug-likeness for most of the compounds. Docking studies were also carried out to investigate the binding affinities as well as interactions of these compounds with the target proteins.
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