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

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

SUBMITTER: Dravyakar BR 

PROVIDER: S-EPMC6446527 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature