碳酰肼
吡唑
咪唑吡啶
化学
吡啶
酶
腙
亚甲基
亚甲基桥
立体化学
分子
组合化学
药物化学
生物化学
有机化学
作者
Devaraj Ganavi,Shashank M. Patil,Vasantha Kumar,Ramith Ramu,Boja Poojary
标识
DOI:10.1002/slct.202300778
摘要
Abstract Diabetic complications poses major threat to mankind which found to be dangerously fatal all over the world. It is thought vital to find new class of molecules to combat diabetic problems. Thus, in continuation of our efforts in identifying new class of α‐glucosidase and α‐amylase inhibitors, a novel series of hybrid molecules comprising of imidazo[1,2‐ a ]pyridine and pyrazoles, i. e. (3‐(Substituted phenyl)‐1H‐pyrazol‐4‐yl)methylene)‐2,7‐dimethyl‐1 H ‐imidazo[1,2‐ a ]pyridine‐3‐carbohydrazide derivatives (8 a – m) were designed through a acyl hydrazone bridge. The compound ( Z )‐N′‐({3‐[4‐(2‐Fluorobenzyloxy)phenyl]‐1 H ‐pyrazol‐4‐ yl }methylene)‐2,7‐dimethyl‐imidazo[1,2‐ a ]pyridine‐3‐carbohydrazide (8 m) emerged as potent inhibitor of α‐glucosidase and α‐amylase enzyme with IC 50 5.00±0.10 μg/mL and 15±0.35 μg/mL respectively. The enzyme kinetics studies revealed reversible non‐competitive mode of inhibition of 8 m against both enzymes. In addition, these compounds were subjected to detailed in‐silico studies to understand their interaction with respective target proteins.
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