Key result
Certain 2-aryl-5-guanidino-1,3,4-thiadiazoles and related iminoimidazolidine derivatives lowered blood pressure in hypertensive rats by a direct relaxant effect on vascular smooth muscle.
Why the study?
Some 2-aryl-5-guanidino-1,3,4-thiadiazoles and analogues were found to lower blood pressure in DOCA hypertensive rats, but their vasodilator activity and structure-activity relationships required further investigation.
These thiadiazole derivatives may identify novel vasodilator leads; leaves open translation to human hypertension therapy.
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.
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Turner et al. (1988) studied Hypertension. 2-aryl-5-guanidino-1,3,4-thiadiazoles was evaluated. Certain 2-aryl-5-guanidino-1,3,4-thiadiazoles and related iminoimidazolidine derivatives lowered blood pressure in hypertensive rats by a direct relaxant effect on vascular smooth muscle.
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