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Synthesis and Biological Activities of Non-Peptide Angiotensin Receptor Antagonists With Tetrazole Replaced Imidazole Ring

Synthesis and Biological Activities of Non-Peptide Angiotensin Receptor Antagonists With Tetrazole Replaced Imidazole Ring

A Wahhab, J Smith, G J Moore

Arzneimittelforschung. 1993 Aug;43(8):828-30.

PMID: 8216436

Abstract:

Angiotensin receptor antagonists related to losartan were synthesized in which the imidazole ring was replaced by tetrazole. 1-[4-(2'-Carboxyphenyl)benzyl]-5-butyl tetrazole and 5-[4-(2'-carboxyphenyl)benzyl]-1-butyl tetrazole had antagonist activities versus angiotensin II in the rat isolated uterus assay of 70% and 10%, respectively, of that of the equivalent imidazole compound 1-[4-(2'-carboxyphenyl)benzyl]-2-butyl imidazole. These data suggest that the antagonist activity of compounds in this class is not dependent on the direction of the heterocyclic ring dipole, and that there is a preference for substitution of the acid group-bearing side-chain at the N atom rather than the C atom of tetrazole.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP114798366	Losartan Related Compound C		114798-36-6	Price

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