Imidazo[4,5-b]pyridine-based AT1 / AT2 angiotensin II receptor antagonists

Abstract The structure-activity relationships of 6-amido-imidazol [4,5-b]pyridine-based angiostensin II antagonists ( V demonstrate that high affinity for the AT 1 and AT 2 receptors is largely dependent upon the R 1 and R 4 substituents. Of this series, L-162,441 and L-162,620 exhibits subnanomolar (IC 50 ) binding affinities to both AT 1 and AT 2 receptors and potent antihypertensive effects in animals upon oral administration.