Medicinal Chemistry

Design, Synthesis, Computer Modeling and Analgesic Activity of Some New Quinazoline Derivatives

Abstract

Helmy Sakr M

Some new 2-(substituted)-N-(6-bromo-4-oxo-2-phenylquinazolin-3(3H)-yl) acetamides (4.1-9), 2-(substituted)- N-(6,8-dibromo-4-oxo-2-phenylquinazolin-3(3H)-yl) acetamides (4.10-18), 2-(substituted)-N-(6-chloro-4-oxo-2- phenylquinazolin-3(3H)-yl) acetamides (4.19-27) and 2-(substituted)-N-(6,8-dichloro-4-oxo-2-phenylquinazolin- 3(3H)-yl) acetamides (4.28-36) were synthesized in good yield and investigated for analgesic activity. Computer aided drug design (CADD) studies were performed to rationalize the best fitting value of the prepared compounds. All the test compounds exhibited significant analgesic activity compared to reference standard diclofenac sodium. The compounds with aliphatic group (CH3 or C2H5) (4.1, 2, 10, 11, 19, 20, 28 and 29) showed most potent analgesic activity of the series and it is moderately more potent compared to the reference standard diclofenac sodium.