Submit Manuscript  

Article Details


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

[ Vol. 18 , Issue. 1 ]

Author(s):

Bhushan R. Dravyakar*, Pramod B. Khedekar, Tabassum Khan, Atul P. Sherje, Kavit N. Patel and Vasanti Suvarna   Pages 4 - 25 ( 22 )

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.

Affiliation:

SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mumbai-400 0056, Computer Aided Drug Design Laboratory, Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur-440 033, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mumbai-400 0056, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mumbai-400 0056, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mumbai-400 0056, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mumbai-400 0056

Graphical Abstract:



Read Full-Text article