[Synthesis and H2-antihistaminic activity of ring methylated metiamide analogues. 4th communication: H2-antihistaminic agents (author's transl)].
In studies on structure-activity relationships of histamine H2-receptor antagonists, the influence of different imidazole ring methylation on the H2-antagonist activity was investigated. 2-Methyl-, 5-methyl-, 2,5-dimethyl- and unsubstituted analogues of metiamide were prepared and tested. While 5-methyl- and unmethylated analogues with a thiourea group proved to be quite active, the 2-methyl- and 2,5-dimethyl-derivatives, as well as those with a urea group, had only low H2-antihistaminic activity.
D000818:Animals; D005260:Female; D005750:Gastric Juice / Q000378:metabolism; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D008785:Metiamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000031:analogs & derivatives*; D014590:Uterine Contraction / Q000187:drug effects
D006635:Histamine H2 Antagonists; D008785:Metiamide; D013890:Thiourea
Synthese und H2-antihistaminische Wirkung ringmethylierter Metiamid-Analoga. 4. Mitteilung: H2-Antihistaminika.