New Benzimidazothiazolone Derivatives as Tyrosinase Inhibitors with Potential Anti-Melanogenesis and Reactive Oxygen Species Scavenging Activities.

ABSTRACT: Thirteen (Z)-2-(substituted benzylidene)benzimidazothiazolone analogs were synthesized and evaluated for their inhibitory activity against mushroom tyrosinase. Among the compounds synthesized, compounds 1-3 showed greater inhibitory activity than kojic acid (IC₅₀ = 18.27 ± 0.89 μM); IC₅₀ = 3.70 ± 0.51 μM for 1; IC₅₀ = 3.05 ± 0.95 μM for 2; and IC₅₀ = 5.00 ± 0.38 μM for 3, and found to be competitive tyrosinase inhibitors. In silico molecular docking simulations demonstrated that compounds 1-3 could bind to the catalytic sites of tyrosinase. Compounds 1-3 inhibited melanin production and cellular tyrosinase activity in a concentration-dependent manner. Notably, compound 2

SUBMITTER: Jung HJ 

PROVIDER: S-EPMC8301170 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature