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Development of selective and reversible pyrazoline based MAO-A inhibitors: Synthesis,biological evaluation and docking studies |
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| Authors: | Muthukumar Karuppasamy Manojkumar Mahapatra Samiye Yabanoglu Gulberk Ucar Barij Nayan Sinha Arijit Basu Nibha Mishra Ashoke Sharon Umasankar Kulandaivelu Venkatesan Jayaprakash |
| Affiliation: | 1. Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835215, India;2. Department of Biochemistry, Faculty of Pharmacy, Hacettepe University, 06100 S?hh?ye, Ankara, Turkey;3. Department of Applied Chemistry, Birla Institute of Technology, Mesra, Ranchi 835215, India;4. Medicinal Chemistry Research Division, Vaagdevi College of Pharmacy, Hanamkonda, Warangal 506001, India |
| Abstract: | 3,5-Diaryl pyrazolines analogs were synthesized and evaluated for their monoamine oxidase (MAO) inhibitory activity. The compounds were found reversible and selective towards MAO-A with selectivity index in the magnitude of 103–105. The docking studies were carried out to gain further structural insights of the binding mode and possible interactions with the active site of MAO-A. Interestingly, the theoretical (Ki) values obtained by molecular docking studies were in congruence with their experimental (Ki) values. |
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