Valsartan, a potent, orally active angiotensin II antagonist developed from the structurally new amino acid series

Abstract Starting from the structure of DuP-753 and a 3-dimensional model of the pentapeptide Tyr-Ile-His-Pro-Ile, a series of new and highly potent antagonists has been designed where the imidazole moiety of the Du Pont compound has been replaced by an N-acylated aminoacid residue. VALSARTAN (Ex. 4e CGP48933, (S)-N-Valeryl-N-[2′-(1H-tetrazol-5-yl-)biphenyl-4-yl]methyl-valine), has been selected for clinical investigation.