-transparent.png){kind=logo}
Nonpeptide angiotensin II receptor antagonists. I. Synthesis and biological activity of pyridine derivatives. 1994
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
Kotobuki Research Laboratories, Kotobuki Pharmaceutical Company, Ltd., Nagano, Japan.
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 )biphenyl-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.
Related Publications
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
June 1993,
Journal of medicinal chemistry,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
July 1993,
Journal of medicinal chemistry,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
April 1993,
Journal of medicinal chemistry,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
March 1997,
Farmaco (Societa chimica italiana : 1989),
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
March 1992,
Journal of medicinal chemistry,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
January 1993,
Journal of medicinal chemistry,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
March 1995,
Chemical & pharmaceutical bulletin,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
August 1990,
American journal of hypertension,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
September 1994,
Nihon yakurigaku zasshi. Folia pharmacologica Japonica,
N Ueyama, and
T Yanagisawa, and
T Kawai, and
M Sonegawa, and
H Baba, and
S Mochizuki, and
K Kosakai, and
T Tomiyama
August 1993,
Tanpakushitsu kakusan koso. Protein, nucleic acid, enzyme,
