[Quinazolinones. 16. Synthesis and in vitro pharmacology of 2-aryl-1- ([3-(imidazol-4-yl)propyl]-guanidinylalkyl)-2,3-dihydro-4(1H)- quinazolinones].
A series of 2-aryl-1- ([3-(imidazol-4-yl)propyl]guanidinylalkyl)-2,3-dihydro-4(1H)- quinazolinones were prepared starting with appropriate aminoalkyl-quinazolinones. The substances proved to be moderate H1-antagonists at the isolated guinea-pig ileum as well as H2-agonists, maximally achieving 1.6 times the activity of histamine at the isolated guinea-pig right atrium. Compounds with a three-membered carbon chain connecting the bicyclus and the guanidine system are up to 100 times more active at the atrium (chronotropic effect) than the corresponding lower homologues.
Büyüktimkin
S
S
Buschauer
A
A
Schunack
W
W
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006146:Guanidines / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis*; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology
D006146:Guanidines; D006634:Histamine H1 Antagonists; D006635:Histamine H2 Antagonists; D007093:Imidazoles; D011799:Quinazolines
Chinazolinone, 16. Mitt. Synthese und in vitro pharmakologie von 2-Aryl-1- ([3-(imidazol-4-yl)propyl]-guanidinoalkyl)-2,3-dihydro-4(1H)- chinazolinonen.