|
|||||
|
|
Pyrazoline based MAO inhibitors: synthesis, biological evaluation and SAR studies |
|
| Authors: | Jagrat Monika Behera Jagannath Yabanoglu Samiye Ercan Ayse Ucar Gulberk Sinha Barij Nayan Sankaran Vadivelan Basu Arijit Jayaprakash Venkatesan |
| Institution: | a Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India b Department of Biochemistry, Faculty of Pharmacy, Hacettepe University, 06100 S?hh?ye, Ankara, Turkey c Informatics, GVK Biosciences Private Limited, 37 Sterling Road, Chennai, India |
| Abstract: | Twenty-two pyrazoline derivatives were synthesized and tested for their human MAO (hMAO) inhibitory activity. Twelve molecules with unsubstituted ring A and substituted ring C (5-16) were found to be potent inhibitors of hMAO-A isoform with SIMAO-A in the order 103 and 104. Ten molecules with unsubstituted ring A and without ring C (21-30), in which eight molecules (21, 23-26, and 28-30) were selective for hMAO-A, one for hMAO-B (22) and the other one non-selective (27). Presence of ring C increases potency as well as SI towards hMAO-A; however its absence decreases both potency and SI towards hMAO-A and hMAO-B. |
| Keywords: | Pyrazolines MAO Selectivity Docking |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |