Synthesis and antihypertensive activity of novel 3-hydrazino-5-phenyl-1,2,4-triazines

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Abstract
To develop antihypertensive agents with peripheral vasodilator activity a series of 40 novel 3-hydrazino-5-phenyl-1,2,4-triazines(II) were synthesized and evaluated in the spontaneously hypertensive rat assay (SHR assay). Based on the performance of the structurally related standard hydralazine (I), 15 triazines were active. Of the hypotensive triazines 13 possessed LD50 values in the mouse greater than I (LD50 = 100 mg/kg); only 1 active triazine had an LD50 value greater than 300 mg/kg (iid). Asymmetric triazines (4) had moderate antihypertensive activity and LD50 values greater than 300 mg/kg (6b, 7c, 8f and 9g). Based on the relationship between toxicity and antihypertensive activity 3 triazines (8f, 9g and 11d) were chosen for dose-response studies in the SHR assay. None were as efficacious as I but all 3 were less toxic, causing similar therapeutic indices relative to I.

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