H2-antagonists: synthesis and activity of 2-amino-5-thiazolyl derivatives |
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Authors: | P V Plazzi F Bordi C Silva G Morini P L Catellani G Vaona M Impicciatore |
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Affiliation: | Istituti di Chimica Farmaceutica, Facoltà di Farmacia, Università di Parma. |
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Abstract: | 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. |
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