In an attempt to discover new potent inhibitors for Mycobacterium tuberculosis (Mtb), a series of 2-(2-hydrazinyl)thiazole derivatives with a wide range of substitutions at 2-, 4- and 5-positions were designed by considering Lipinski rule. The designed compounds were synthesized, characterized and evaluated for their inhibitory potential against Mtb, H₃₇Rv, by in vitro assay. The compounds, ethyl-4-methyl-2-[(E)-2-[1-(pyridin-2-yl)ethylidene]hydrazin-1-yl]-1,3-thiazole-5-carboxylate, 4d, and ethyl-2-[(E)-2-[(2-hydroxyphenyl)methylidene]hydrazin-1-yl]-4-methyl-1,3-thiazole-5-carboxylate, 2i showed noticeable inhibitory activity against Mtb, H₃₇Rv with minimum inhibitory concentration (MIC) of 12.5 μM and 25 μM respectively. An attempt has been made to understand the mechanism of action by binding interactions of these molecules with β-ketoacyl-ACP synthase protein through docking studies. The inhibition constants for compounds 4d and 2i were found to be 1.46 μM and 0.177 μM respectively.

为了发现新的有效的结核分枝杆菌抑制剂（Mtb），通过考虑Lipinski规则设计了一系列在2-，4-和5-位具有广泛取代基的2-（2-肼基）噻唑衍生物。通过体外测定合成，表征并评估了设计的化合物对Mtb，H ₃₇ Rv的抑制潜力。化合物4-甲基-2-[[（E）-2- [1-（吡啶-2-基）亚乙基]肼基-1-基] -1,3-噻唑-5-羧酸乙酯，4d和2-[（E）-2-[（2-羟基苯基）亚甲基]肼-1-基] -4-甲基-1,3-噻唑-5-羧酸乙酯，2i分别显示出对Mtb和H ₃₇ Rv的显着抑制活性，最小抑制浓度（MIC）分别为12.5μM和25μM。通过对接研究，已经尝试通过使这些分子与β-酮酰基-ACP合酶蛋白结合相互作用来理解作用机理。发现化合物4d和2i的抑制常数分别为1.46μM和0.177μM。