Design and Development of Novel 2-(Morpholinyl)-N-substituted Phenylquinazolin-4-amines as Selective COX-II Inhibitor

Author(s): Bhushan R. Dravyakar*, Pramod B. Khedekar, Tabassum Khan, Atul P. Sherje, Kavit N. Patel, Vasanti Suvarna.

Journal Name: Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents)

Volume 18 , Issue 1 , 2019

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Graphical Abstract:


Background: A novel series of 2-(Morpholin-4-yl)-N-phenylquinazolin-4- amine derivatives were synthesized and confirmed with spectral and elemental techniques.

Methods: The compounds were tested for analgesic and anti-inflammatory activity by various pain models in rodents whereas the selectivity towards COX-2 receptor is determined by in vitro assay.

Results: Screening results of compounds exhibited comparable biological activity with that of standard compound Indomethacin used for study. Compound 5d was found to be significantly potent with respect to its anti-inflammatory and analgesic activity with substantial COX-II selectivity.

Conclusion: In silico analysis by molecular docking and 3D-QSAR studies justifies activity profile of compound 5d, suggesting that it may have potential for further evaluation and development as lead molecule for therapy in pain management.

Keywords: 3D-QSAR, analgesic, anti-inflammatory, COX II inhibitor, molecular docking, quinazoline.

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Article Details

Year: 2019
Page: [4 - 25]
Pages: 22
DOI: 10.2174/1871523017666181022144053

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