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.