New class of thio/semicarbazide-based benzyloxy derivatives as selective class of monoamine oxidase-B inhibitors.

ABSTRACT: Sixteen thio/semicarbazide-based benzyloxy derivatives (BT1-BT16) were synthesized and evaluated for their inhibitory activities against monoamine oxidases (MAOs). Most compounds showed better inhibitory activity against MAO-B than against MAO-A. BT1, BT3, and BT5 showed the greatest inhibitory activity with an identical IC₅₀ value of 0.11 µM against MAO-B, followed by BT6 and BT7 (IC₅₀ = 0.12 µM) and BT2 (IC₅₀ = 1.68 µM). The selectivity index of BT5 was the highest (363.64) for MAO-B, whereas that of BT1 was 88.73. BT1 and BT5 were reversible MAO-B inhibitors, based on the results of dialysis experiments. In inhibition kinetics, BT1 and BT5 were competitive MAO-B inhibitors with K_i values of 0.074 ± 0.0020 and 0.072 ± 0.0079 µM, respectively. A

SUBMITTER: Chandran N 

PROVIDER: S-EPMC11682371 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature