QUINAZOLINONES .18. SYNTHESIS AND H1/H2-ANTIHISTAMINIC ACTIVITY OF OMEGA-[2-ARYL-2,3-DIHYDRO-4(1H)-QUINAZOLINON-1-YL]ALKYL-SUBSTITUTED UREAS AND CYANOGUANIDINES

Abstract

A series of (2-aryl-2,3-dihydro-4(1H)-quinazolinon-1-yl)alkyl-substituted cyanoguanidines and ureas with histamine, cimetidine or roxatidine partial structure was prepared and tested for H-1- and H-2-antagonism at the isolated ileum and the isolated right atrium of the guinea-pig. All compounds investigated were only very weak H-1-antagonists, whereas the 3-[3-(1-piperidinylmethyl)phenoxy]propyl-cyanoguanidines and -ureas were more potent H-2-antagonists than cimetidine, maximally achieving about ranitidine's potency.