Synthesis and Evaluation of Novel Nonpeptide Angiotensin II Receptor Antagonists : Imidazo[4,5-c]pyridine Derivatives with an Aromatic Substituent

概要

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Starting from recently reported nonpeptidic angiotensin II (AII) receptor antagonists, we have designed and prepared a new series of 6-arylimidazo[4,5-c]pyridine derivatives. Variation of phenyl groups at the 4-, 6- or 7-position of imidazo[4,5-c]pyridine showed that substitution at the 6-position resulted in receptor-binding activity almost as potent as that of DuP 753. This led to synthesis and evaluation of an extensive series of 6-aryl-imidazo[4,5-c]pyridine derivatives. Some of them were 4-fold more potent in vitro than DuP 753,but only showed weak antihypertensive activity in vivo when given orally to rats.
社団法人日本薬学会の論文
1995-03-15