SYNTHESIS OF PHENOXYACETIC ACID-DERIVATIVES AS HIGHLY POTENT ANTAGONISTS OF GASTRIN CHOLECYSTOKININ-B RECEPTORS - II/

Authors
TAKEDA Y KAWAGOE K YOKOMIZO A YOKOMIZO Y HOSOKAMI T SHIMOTO Y TABUCHI Y OGIHARA Y OTSUBO R HONDA Y YOKOHAMA S
Citation
Y. Takeda et al., SYNTHESIS OF PHENOXYACETIC ACID-DERIVATIVES AS HIGHLY POTENT ANTAGONISTS OF GASTRIN CHOLECYSTOKININ-B RECEPTORS - II/, Chemical and Pharmaceutical Bulletin, 46(6), 1998, pp. 951-961
Citations number
30
Categorie Soggetti
Chemistry Medicinal",Chemistry,"Pharmacology & Pharmacy
Journal title
Chemical and Pharmaceutical Bulletin → ACNP
ISSN journal
00092363
Volume
46
Issue
6
Year of publication
1998
Pages
951 - 961
Database
ISI
SICI code
0009-2363(1998)46:6<951:SOPAAH>2.0.ZU;2-F
Abstract
A series of phenoxyacetanilide derivatives was synthesized and their a ntagonist activities for human gastrin/cholecystokinin (CCK)-B and CCK -A receptors were evaluated. Among the compounds synthesized, bamoylme thyl)carbamoylmethyl]-ureido]phenyl]acetic acid (20i, DA-3934) exhibit ed high affinity for gastrin/CCK-B receptors and high selectivity over CCK-A receptors. DA-3934 and its methyl ester derivative inhibited pe ntagastrin-induced gastric acid secretion in rats in a dose-dependent manner.