New quinoline-thiolactone conjugates as potential antitubercular and antibacterial agents

Abstract

Tuberculosis and bacterial infections are major challenges because of elevated infection rates and drug resistance. New chemical agents need to be developed to address them. Thiolactomycin and quinolines are promising lead molecules in the design of new antitubercular and antibacterial agents. Herein, we report the design and synthesis of series of new quinoline-thiolactone conjugates as potential antitubercular and antibacterial agents. Two of the conjugates, 6b and 6d, exhibited good antitubercular activity with MIC value of 8 µg/mL. Docking studies showed that the conjugates, 6b and 6d, exhibited good binding affinity towards the target protein KasA of M. tuberculosis. Two other conjugates also showed decent antibacterial activity with MIC value of 8 µg/mL. Further, the docking of conjugate 7a was better than standard drug, linezolid against three different molecular receptors.