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Anti‐Inflammatory, Analgesic Evaluation and Molecular Docking Studies of N‐Phenyl Anthranilic Acid‐Based 1,3,4‐Oxadiazole Analogues
Author(s) -
Suman Bala,
Sunil Kamboj,
Vipin Saini,
D.N. Prasad
Publication year - 2013
Publication title -
journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.436
H-Index - 50
eISSN - 2090-9063
pISSN - 2090-9071
DOI - 10.1155/2013/412053
Subject(s) - chemistry , anthranilic acid , oxadiazole , docking (animal) , analgesic , carrageenan , enzyme , cyclooxygenase , stereochemistry , pharmacology , anti inflammatory , edema , combinatorial chemistry , biochemistry , organic chemistry , medicine , psychology , nursing , psychiatry
A novel series of N-phenyl anthranilic acid-based 1,3,4-oxadiazoles were prepared (4a–h) and subjected to anti-inflammatory, analgesic activity and molecular docking studies to target cyclooxygenase-2 enzyme. 1,3,4-Oxadiazole derivatives were screened for anti-inflammatory activity in carrageenan-induced rat paw edema and analgesic activity by tail immersion method. In synthesized compounds, the free carboxylic group, which is responsible for gastric side effects, was derivatized by heterocyclic 1,3,4-oxadiazole bioactive core, which showed good interaction with COX-2 receptor with good docking score. Among all the synthesized compounds, 4e and 4f have emerged out as potential COX-2 inhibitors

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