| Literature DB >> 3361579 |
S Turner1, M Myers, B Gadie, S A Hale, A Horsley, A J Nelson, R Pape, J F Saville, J C Doxey, T L Berridge.
Abstract
Some 2-aryl-5-guanidino-(or N-substituted guanidino)-1,3,4-thiadiazoles and closely related analogues were found to lower blood pressure in metacorticoid (DOCA) hypertensive rats. In the unsubstituted guanidines that exhibited low toxicity, optimum activity resulted when the aryl group was a 2-methylphenyl ring (11). Modifications to the guanidine group did not increase antihypertensive activity, but, in the 2-methylphenyl series, the N-n-butyl- and N-(2-methoxyethyl)guanidines (63 and 78) and the related iminoimidazolidine 93 were of comparable activity to that of the unsubstituted guanidine 11. The iminoimidazolidine 93 showed a somewhat longer duration of action than the guanidine derivatives. Preliminary studies in a pithed rat preparation indicated that these thiadiazole derivatives (11, 63, and 93) lowered blood pressure by a direct relaxant effect on vascular smooth muscle.Entities:
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Year: 1988 PMID： 3361579 DOI： 10.1021/jm00400a004
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446