Design, synthesis, and biological evaluation of oxindole derivatives as antidepressive agents

Sharad Kumar Suthar, Sumit Bansal, Md Maqusood Alam, Varun Jaiswal, Amit Tiwari, Anil Chaudhary, Angel Treasa Alex, Alex Joseph

Research output: Contribution to journalArticle

9 Citations (Scopus)

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 μmol, whereas the reference drug moclobemide displayed an IC50 of 13.1 μmol. 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.

Original languageEnglish
Pages (from-to)5281-5285
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number22
DOIs
Publication statusPublished - 15-11-2015

Fingerprint

Imipramine
Monoamine Oxidase
Antidepressive Agents
Inhibitory Concentration 50
Assays
Moclobemide
Hindlimb Suspension
Derivatives
Suspensions
Atoms
Pharmaceutical Preparations
oxindole
Swimming

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Suthar, Sharad Kumar ; Bansal, Sumit ; Alam, Md Maqusood ; Jaiswal, Varun ; Tiwari, Amit ; Chaudhary, Anil ; Alex, Angel Treasa ; Joseph, Alex. / Design, synthesis, and biological evaluation of oxindole derivatives as antidepressive agents. In: Bioorganic and Medicinal Chemistry Letters. 2015 ; Vol. 25, No. 22. pp. 5281-5285.
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Design, synthesis, and biological evaluation of oxindole derivatives as antidepressive agents. / Suthar, Sharad Kumar; Bansal, Sumit; Alam, Md Maqusood; Jaiswal, Varun; Tiwari, Amit; Chaudhary, Anil; Alex, Angel Treasa; Joseph, Alex.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 25, No. 22, 15.11.2015, p. 5281-5285.

Research output: Contribution to journalArticle

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