Synthesis of new derivatives containing pyridine, investigation of MAO inhibitory activities and molecular docking studies

Author:

Osmaniye Derya12ORCID,Sağlık Begüm Nurpelin12ORCID,Levent Serkan12,Özkay Yusuf12,Kaplancıklı Zafer Asım1,Turan Gülhan1

Affiliation:

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Anadolu University , 26470 Eskişehir , Turkey

2. Central Analysis Laboratory, Faculty of Pharmacy , Anadolu University , 26470 Eskişehir , Turkey

Abstract

Abstract In this study, novel pyridine-containing thiazolyl hydrazone derivatives were synthesized. Structure determinations of the compounds were performed using 1H NMR, 13C NMR and HRMS techniques. The biological activities of the compounds were evaluated against MAO enzymes by in vitro fluorometric method. As a result of activity studies, compound 3a showed selective inhibitory activity against MAO-B enzyme with IC50 = 0.088 + 0.003 µM. The selectivity index of this compound is greater than 1136. Molecular docking studies were carried out using 2V5Z crystal. It has been observed that docking studies and activity studies are in harmony.

Publisher

Walter de Gruyter GmbH

Subject

General Biochemistry, Genetics and Molecular Biology

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