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.
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.
Barocelli
E
E
Department of Pharmacy, University of Parma, Italy.
Chiavarini
M
M
Morini
G
G
Plazzi
P V
PV
Vitali
T
T
Impicciatore
M
M
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*
D006635:Histamine H2 Antagonists; D013844:Thiazoles