Design, Synthesis, and Biological Evaluation of Oxindole Derivatives as Antidepressive Agents

Suthar, Sharad Kumar and Bansal, Sumit and Tiwari, Amit and Chaudhary, Anil and Alex, Angel Treasa and Joseph, Alex (2015) Design, Synthesis, and Biological Evaluation of Oxindole Derivatives as Antidepressive Agents. Bioorganic & Medicinal Chemistry Letters, 25. pp. 5281-5285.

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Abstract

The 3-substituted oxindole derivatives were designed, synthesized, and evaluated for antidepressant activity by employing forced swimming test, tail suspension test, and MAO-A inhibition assay. Results of biological studies revealed that the majority of compounds exhibited potent to moderately potent activity and among them, 12 displayed potency comparable to that of the imipramine with %DID of 37.95 and 44.84 in the FST and TST, respectively. At the same time, imipramine showed %DID of 43.62 and 50.64 in the FST and TST, correspondingly. In the MAO-A inhibition assay, 12 showed an IC50 of 18.27 lmol, whereas the reference drug moclobemide displayed an IC50 of 13.1 lmol. The SAR study disclosed that the presence of bromo atom at the phenyl/furanyl or thienyl moiety in the oxindole derivatives was critical for the antidepressant activity.

Item Type: Article
Uncontrolled Keywords: Oxindole derivatives; Antidepressant activity; MAO-A inhibitors; Forced swimming test; Tail suspension test
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Biotechnology
Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Library
Date Deposited: 31 Dec 2015 08:58
Last Modified: 31 Dec 2015 08:58
URI: http://eprints.manipal.edu/id/eprint/144977

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