ACIDIC PHENOLS - A NEW CLASS OF POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

A series of imidazo[4,5-b]pyridine-based acidic phenols (Table 1,2) an d biphenyl ethers (Table 3) are exemplified as novel non-peptide AII r eceptor antagonists. o,o'-substituents which affect the acidity of the phenolic portion dramatically impact the activity of the compounds. T he most potent antagonist in this series (Compound 13, IC50 5 nM, rabb it aorta) exhibited good in vivo potency after both iv and oral admini stration to conscious rats.