6-Arylamino-5,8-quinazolinediones as potent inhibitors of endothelium-dependent vasorelaxation

Abstract

6-(Substituted-phenyl)amino-5,8-quinazolinediones (3) were synthesised by regioselective substitution of 5,8-quinazolinedione (5) with appropriate arylamines in the presence of Ce(III) ions. All synthesised 5,8-quinazolinediones 3 showed a potent and efficacious inhibitory effect on the acetylcholine (ACh)-induced vasorelaxation of rat aorta with the endothelium. The quinones 3, at a low concentration of 0.1 μM, reduced the maximal response with increase of EC50 values for ACh. The results indicate that quinones 3 are potent inhibitors of endothelium-dependent vasorelaxation. © 2002 Éditions scientifiques et médicales Elsevier SAS. All rights reserved.