Development of highly potent melanogenesis inhibitor by in vitro, in vivo and computational studies.

ABSTRACT: The present work describes the synthesis of few hydroxylated amide derivatives as melanogenesis inhibitors. In vitro, in vivo and computational studies proved that compound 6d is a highly potent melanogenesis inhibitor compared to standard kojic acid. The title amides 4a-e and 6a-e were synthesized following simple reaction routes with excellent yields. Most of the synthesized compounds exhibited good mushroom tyrosinase inhibitory activity, but compound 6d showed excellent activity (IC₅₀ 0.15 µM) compared to standard kojic acid (IC₅₀ 16.69 µM). Lineweaver-Burk plots were used for the determination of kinetic mechanism, and it was found that compounds 4c and 6d showed non-competitive inhibition while 6a an

SUBMITTER: Abbas Q 

PROVIDER: S-EPMC5503496 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature