Discovery and development of novel rhodanine derivatives targeting enoyl-acyl carrier protein reductase

A series of rhodanine derivatives RB1-RB23 were synthesized through a two-round screening. Their Mycobacterial tuberculosis (Mtb) InhA inhibitory activity and Mtb growth blocking capability were evaluated. The most potent hit compound RB23 indicated comparable InhA inhibiton (IC50 = 2.55 μM) with the positive control Triclosan (IC50 = 6.14 μM) and Isoniazid (IC50 = 8.29 μM). Its improved growth-blocking effect on Mtb and low toxicity were...