Abstract
AbstractA series of pyrrole‐thiazolidin‐4‐one conjugates were synthesized and evaluated for their anti‐mycobacterial and anti‐bacterial activities. Two compounds, 10 a and 10 k, were the most effective conjugates and produced identical MICs (0.5 μg/mL) against M. tuberculosis H37Rv with a high selectivity index. Upon evaluation against the ESKAP bacteria panel, compound 10 g emerged most effective against S. aureus (MIC=8.0 μg/mL) while compound 10 o produced activity against A. baumannii (MIC=4.0 μg/mL). A molecular docking study revealed that the most active compound 10 a has similar binding interactions as those of BM212 and rimonabant, with a comparable docking score against M. tuberculosis mycolic acid transporter MmpL3.
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