Synthesis and Antiinflammatory Activity of 2,3‐Diaryl‐4(3H)‐quinazolinones.

Abstract

Fused pyrimidine derivatives R 0515Synthesis and Antiinflammatory Activity of 2,3-Diaryl-4(3H)-quinazolinones. -Eighteen title compounds of type (VI) or (VIII) are prepared and evaluated for their cyclooxygenase-2 inhibitory activities by the colorimetric COX (ovine) inhibitor and for their antiinflammatory activities. Compound (VIc) is found to be the most potent COX-2 inhibitor and exhibits mild antiinflammatory effects. -(YADAV, M. R.; SHIRUDE, S. T.; PARMAR, A.; BALARAMAN, R.; GIRIDHAR, R.; Chem.

An experimental investigation of substituent effects on the formation of 2,3-dihydroquinazolin-4(1H)-ones: a kinetic study

“…2,3‐Dihydroquinazolin‐one derivatives have been reported to possess a wide range of pharmacological activities such as anti‐inflammatory and analgesic activities and antitumor, anticancer, antibacterial, and diuretic activities . The unique biological activities have made quinazolinone synthetic studies over the years very attractive . These compounds could be synthesized by different methods in that the general method includes condensation of aldehydes or ketones with 2‐amino‐benzamide in the presence of acid catalysts, such as Sc(OTf) 3 , NH 4 Cl, p ‐TsOH, CuCl 2 , and [Bmim]PF6 .…”

Pentafluorophenylammonium triflate-CuCl2: A mild, efficient and reusable heterogeneous catalyst system for facile synthesis of 4(3H)-quinazolinones under solvent-free conditions

“…4(3H)-quinazolinones are an important class of fused heterocycles with a wide range of pharmacological and biological activities such as antagonist, 1 antimalarial, 2 antitumour, 3 antibacterial, 4 anti-inflammatory, 5 insecticidal, and antimicrobial activity. 6 In addition, quinazolinone moiety is a building block for approximately 150 naturally occurring alkaloids, such as glycosminine, 7 deoxyvasicinone, 8 and drugs like methaqualone 9 and piriqualone.…”