-transparent.png){kind=logo}
In search for inhibitors of gastric H+/K+-ATPase, 4-(phenylamino)quinoline-3-carboxamides were synthesized and evaluated for antisecretory activity against histamine-induced gastric acid secretion in rats. These compounds were synthesized by condensation of aniline derivatives with N-substituted 4-chloroquinoline-3-carboxamides, which were obtained from treatment of 4(1H)-quinolinone-3-carboxylic acid with thionyl chloride. Most of the compounds inhibited histamine-induced gastric acid secretion in rats. Among them, N-allyl-4-(2-ethylphenylamino)quinoline-3-carboxamide (4h) was the most potent inhibitor and had the best profile as a candidate antiulcer agent. This compound showed reversible, K+-competitive gastric H+/K+-ATPase inhibitory activity.
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
September 1992,
Journal of medicinal chemistry,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
December 2013,
Archiv der Pharmazie,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
June 1997,
Chemical & pharmaceutical bulletin,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
January 1994,
Progress in medicinal chemistry,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
April 2019,
Bioorganic & medicinal chemistry,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
July 1997,
Chemical & pharmaceutical bulletin,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
May 2014,
European journal of medicinal chemistry,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
December 2017,
Bioorganic chemistry,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
January 1996,
Journal of medicinal chemistry,
M Uchida, and
K Otsubo, and
J Matsubara, and
T Ohtani, and
S Morita, and
K Yamasaki
April 1974,
The Journal of organic chemistry,
