Chemical and Pharmaceutical Bulletin p. 1841 - 1849 (1994)
Update date:2022-08-03
Topics:
Ueyama
Yanagisawa
Kawai
Sonegawa
Baba
Mochizuki
Kosakai
Tomiyama
Substituted pyridines were synthesized as potential angiotensin II (AII) receptor antagonists. Substitution at the position 2 in the pyridine resulted in potent activity, and the optimal alkyl length was four carbons. The potency further increased with the introduction of a hydroxymethyl group at the position 4. One of the compounds, 2-butyl-6-chloro-4-hydroxymethyl-5-methyl-3-[[2'-(1H-tetrazol-5-yl)bip henyl-4-yl]methyl]pyridine 9 h (KT3-579)is a competitive AII antagonist with a pA2 value of 9.31, and is about 10 times more potent than Du Pont 753. It was found to be an AT1 specific antagonist with an IC50 of 3.09 nM.
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(1995)
