title: H2-receptor antagonist activity of N-methylthiourea, N-cyano-N'-methylguanidine, N-cyanoamidine, N-carbamoylamidine and N-sulfamoylamidine 5-substituted thiazole derivatives on guinea-pig atria.
abstract: The H2-antagonist activity of thiazole derivatives, substituted on position 5 with urea-equivalent groups, has been tested on guinea-pig isolated atria stimulated by dimaprit. By comparing the activities of the 2,5-disubstituted thiazole derivatives with those of the corresponding 2,4-disubstituted derivatives it can be seen that the side-chain position is critical to activity and differently influences activity in the various series. The heteroaromatic ring atom sequence N-C-S-C-side chain is always associated with a low antagonist activity.
authors.affiliation: Department of Pharmacy, University of Parma, Italy.
authors.forename: E
authors.initials: E
authors.lastname: Barocelli
authors.forename: M
authors.initials: M
authors.lastname: Chiavarini
authors.forename: G
authors.initials: G
authors.lastname: Morini
authors.forename: P V
authors.initials: PV
authors.lastname: Plazzi
authors.forename: T
authors.initials: T
authors.lastname: Vitali
authors.forename: M
authors.initials: M
authors.lastname: Impicciatore
mesh_terms: D000818:Animals; D016275:Atrial Function; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects*; D006635:Histamine H2 Antagonists; D066298:In Vitro Techniques; D008297:Male; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology*
chemical_list: D006635:Histamine H2 Antagonists; D013844:Thiazoles