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

被引：0
|
作者：
Osmaniye, Derya [1 ,2 ]
Saglik, Begum Nurpelin [1 ,2 ]
Levent, Serkan [1 ,2 ]
Ozkay, Yusuf [1 ,2 ]
Kaplancikli, Zafer Asim [1 ]
Turan, Gulhan [1 ]
机构：
[1] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey
[2] Anadolu Univ, Fac Pharm, Cent Anal Lab, TR-26470 Eskisehir, Turkey
来源：
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES | 2022年 / 77卷 / 11-12期
关键词：
molecular docking; pyridine; selective MAO-B inhibitor; thiazolyl-hydrazone; MONOAMINE-OXIDASE-A; BIOLOGICAL EVALUATION; THIAZOLE DERIVATIVES; RAT-BRAIN; DESIGN; IDENTIFICATION; HYDRAZONE; ALANINE; AMINES;
D O I：
10.1515/znc-2022-0075
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
In this study, novel pyridine-containing thiazolyl hydrazone derivatives were synthesized. Structure determinations of the compounds were performed using H-1 NMR, C-13 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 mu M. 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.
引用
收藏
页码：509 / 517
页数：9
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