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α‐Glucosidase Inhibition by Usnic Acid Derivatives by Huy Truong Nguyen; Asshaima Paramita Devi; Tran‐Van‐Anh Nguyen; Warinthorn Chavasiri; Duc‐Dung Pham; Jirapast Sichaem; Ngoc‐Hong Nguyen; Bui‐Linh‐Chi Huynh; Van‐Kieu Nguyen; Thuc Huy Duong is a Agricultural and Biological Sciences article available to read on EtoBox.

What is α‐Glucosidase Inhibition by Usnic Acid Derivatives about?

## Abstract This study investigated a set of new potential antidiabetes agents. Derivatives of usnic acid were designed and synthesized. These analogs and nineteen benzylidene analogs from a previous study were evaluated for enzyme inhibition of α‐glucosidase. Analogs synthesized using the Dakin oxidative method displayed stronger activity than the pristine usnic acid (IC~50~>200 μM). Methyl (2E,3R)‐7‐acetyl‐4,6‐dihydroxy‐2‐(2‐methoxy‐2‐oxoethylidene)‐3,5‐dimethyl‐2,3‐dihydro‐1‐benzofuran‐3‐carboxylate (6b) and 1,1′‐(2,4,6‐trihydroxy‐5‐methyl‐1,3‐phenylene)di(ethan‐1‐one) (6e) were more potent than an acarbose positive control (IC~50~ 93.6±0.49 μM), with IC~50~ values of 42.6±1.30 and 90.8±0.32 μM, respectively. Most of the compounds synthesized from the benzylidene series displayed promising activity. (9bR)‐2,6‐Bis[(2E)‐3‐(2‐chlorophenyl)prop‐2‐enoyl]‐3,7,9‐trihydroxy‐8,9b‐dimethyldibenzo[b,d]furan‐1(9bH)‐one (1c), (9bR)‐3,7,9‐trihydroxy‐8,9b‐dimethyl‐2,6‐bis[(2E)‐3‐phenylprop‐2‐enoyl]dibenzo[b,d]furan‐1(9bH)‐one (1g), (9bR)‐2‐acetyl‐6‐[(2E)‐3‐(2‐chlorophenyl)prop‐2‐enoyl]‐3,7,9‐trihydroxy‐8,9b‐dimethyldibenzo[b,d]furan‐1(9bH)‐one (2d), (9bR)‐2‐acetyl‐6‐[(2E)‐3‐(3‐chlorophenyl)pro

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Author

Huy Truong Nguyen; Asshaima Paramita Devi; Tran‐Van‐Anh Nguyen; Warinthorn Chavasiri; Duc‐Dung Pham; Jirapast Sichaem; Ngoc‐Hong Nguyen; Bui‐Linh‐Chi Huynh; Van‐Kieu Nguyen; Thuc Huy Duong

Publisher

Wiley

Published

2021

Language

EN

Field

Agricultural and Biological Sciences (Life Sciences)