Synthesis and evaluation of substituted 1,2,4 triazolinone derivatives as novel angiotensin II receptor antagonists as antihypertensive agents

A set of substituted 1,2, 4 triazolinone derivatives have been synthesized as novel angiotensin II (Ang II) receptor antagonists as antihypertensive agents. Systematic variation of the substituents at the ortho position of N- aryl triazolinones resulted in six novel compounds. The compounds have been evaluated in vivo antihypertensive activity via acute renal hypertension model. Amongst the sixcompounds synthesized two compounds were found to possess promising antihypertensive activity. Compounds TZN1 and TZN4 emerged as maximally active compounds comparable to Losartan and Telmisartan which are a prototype for this class of drugs. A receptor binding model is also proposed on the basis on the basis of structure–activity relationship in this study.
Author(s): Anupama Paratea, Rajesh Sharma and Subhash Chandra Chaturvedi

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