H2-antagonists: synthesis and activity of 2-amino-5-thiazolyl derivatives.
2-Amino- and 2-guanidinothiazole derivatives having in position 5 a methylthioalkyl side-chain with urea-equivalent moieties were prepared for comparison with H2-antagonists of cimetidine and tiotidine series. Examination of the pharmacological results obtained from experiments on guinea pig atria and in cat gastric fistula, suggests some general observations about the structure-activity relationship of the compounds synthesized. The activity trend of these products is different from that of H2-imidazole antagonists while it is similar to that of the tiotidine series. Unlike the tiotidine similar compounds, the 2-guanidino-5-thiazolyl derivatives are less potent than the corresponding 2-amino-5-thiazolyl products. The activity of the latter ones is reduced in comparison to that of tiotidine or cimetidine.
Plazzi
P V
PV
Istituti di Chimica Farmaceutica, Facoltà di Farmacia, Università di Parma.
Bordi
F
F
Silva
C
C
Morini
G
G
Catellani
P L
PL
Vaona
G
G
Impicciatore
M
M
D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D002415:Cats; D055598:Chemical Phenomena; D002621:Chemistry; D017259:Dimaprit; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D009200:Myocardial Contraction / Q000187:drug effects; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013890:Thiourea / Q000494:pharmacology
D000588:Amines; D006635:Histamine H2 Antagonists; D013844:Thiazoles; D013890:Thiourea; D017259:Dimaprit