Synthesis and Evaluation of Human Monoamine Oxidase Inhibitory Activities of Some 3,5‐Diaryl‐N‐substituted‐4,5‐dihydro‐1H‐pyrazole‐1‐carbothioamide Derivatives

• DOI: 10.1002/ardp.201100448
• Publication Date: 2012-06-05T15:23:34Z
• Authors: Kerem Şentürk; Oya Unsal Tan; Samiye Yabanoğlu ...; Gülberk Uçar; Erhan Palaska
• Keywords: Pyrazole; Monoamine oxidase B

Sixteen 3-aryl-5-(4-fluorophenyl)-N-substituted-4,5-dihydro-1H-pyrazole-1-carbothioamide derivatives were synthesized and their structure identified by UV, IR, (1) H NMR, mass spectra, microanalyses. The compounds evaluated in vitro for human monoamine oxidase (hMAO) inhibitory activities MAO-A -B selectivity. All the found to potently inhibit isoforms. 5-(4-Fluorophenyl)-3-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide (1.0 × 10(-3) µM) was hMAO-A most selectively potently. binding mode of 5-(4-fluorophenyl)-3-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide also predicted using docking studies.