Design, synthesis, and biological activity of certain quinazolinedione derivatives as potent phosphodiestrase4 inhibitors

Citation:
Elansary, A. K., H. H. Kadry, E. M. Ahmed, and A. S. M. Sonousi, "Design, synthesis, and biological activity of certain quinazolinedione derivatives as potent phosphodiestrase4 inhibitors", Medicinal Chemistry Research, vol. 21, issue 11, pp. 3557 - 3567, 2012.

Abstract:

In this study, a series of 3-butylquinazolinedione linked with different substituent to N1 of quinazoline nucleus have been synthesized. Some of the new final compounds tested in vitro for their inhibitory activity against phosphodiestrase 4B which is the enzyme responsible for the hydrolysis of cyclic adenosine mono phosphate, the second messenger involved in the regulation of important cell functions. Compound 7f (100%) showed inhibition better than rolipram (90%), while the other tested compounds showed moderate activity. Docking study has been done to rationalize the obtained biological results.

Notes:

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