Ontology highlight
ABSTRACT:
SUBMITTER: Shalaby R
PROVIDER: S-EPMC6442233 | biostudies-literature | 2019 Dec
REPOSITORIES: biostudies-literature
Shalaby Raed R Petzer Jacobus P JP Petzer Anél A Ashraf Usman M UM Atari Ealla E Alasmari Fawaz F Kumarasamy Sivarajan S Sari Youssef Y Khalil Ashraf A
Journal of enzyme inhibition and medicinal chemistry 20191201 1
The present study describes the synthesis of a series of 22 chalcone analogs. These compounds were evaluated as potential human MAO-A and MAO-B inhibitors. The compounds showed varied selectivity against the two isoforms. The IC<sub>50</sub> values were found to be in the micromolar to submicromolar range. The K<sub>i</sub> values of compound 16 were determined to be 0.047 and 0.020 μM for the inhibition of MAO-A and MAO-B, respectively. Dialysis of enzyme-inhibitor mixtures indicated a reversib ...[more]