Ontology highlight
ABSTRACT:
SUBMITTER: Nath C
PROVIDER: S-EPMC6071705 | biostudies-literature | 2018 Jul
REPOSITORIES: biostudies-literature
Nath Chandrani C Badavath Vishnu Nayak VN Thakur Abhishek A Ucar Gulberk G Acevedo Orlando O Mohd Siddique Mohd Usman MU Jayaprakash Venkatesan V
MedChemComm 20180608 7
A series of 2-methoxy-4-(5-phenyl-4,5-dihydro-1<i>H</i>-pyrazol-3-yl)phenol (pyrazoline) derivatives (<b>2-6</b>) have been synthesized and tested for human monoamine oxidase (hMAO) inhibitory activity. The most active derivative (<b>2</b>) behaved as a competitive hMAO-A inhibitor, with an inhibition constant value of 0.08 μM and a strong hMAO-A selectivity (<i>K</i><sub>i</sub>(hMAO-B)/<i>K</i><sub>i</sub>(hMAO-A) > 1751). In addition, <b>2</b> exhibited little to no cytotoxic effects up to a ...[more]