[Quinazolinones. 18. Synthesis and H1/H2-antihistaminic action of omega-[2-aryl-2,3-dihydro-4(1H)-quinazolinone-1-yl]alkyl substituted ureas and cyanoguanidines].
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 H1- and H2-antagonism at the isolated ileum and the isolated right atrium of the guinea-pig. All compounds investigated were only very weak H1-antagonists, whereas the 3-[3-(1-piperidinyl-methyl)phenoxy]propyl-cyanoguanidines and -ureas were more potent H2-antagonists than cimetidine, maximally achieving about ranitidine's potency.
Fakultät für Pharmazie, Universität Istanbul, Türkei.
S
S
Büyüktimkin
A
A
Buschauer
W
W
Schunack
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis*; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D009206:Myocardium / Q000378:metabolism; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D006146:Guanidines; D006634:Histamine H1 Antagonists; D006635:Histamine H2 Antagonists; D011799:Quinazolines; D014508:Urea
Chinazolinone, 18. Mitt.: Synthese und H1/H2-antihistaminische Wirkung omega-[2-aryl-2,3-dihydro-4(1H)-chinazolinon-1-yl]alkyl-substituierter Harnstoffe und Cyanoguanidine.