Abstract
Pyridine isomers replacing the tetrazole-bearing phenyl of the angiotensin II antagonist L-158,338 were prepared. The 4-phenyl-3-tetrazolylpyridyl isomer (compound 3 ) exhibited low nanomolar binding affinity to the AT 1 receptor. Other isomers prepared were 60 to 100 - fold less active compared to L-158,338. Compound 3 is orally active is rats at 1 mg/kg, but the IV vs. PO activites indicated a somewhat poorer oral bioavailability than that of L-158,338.
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