2. Academic Validation
  3. Synthesis of phenoxyacetic acid derivatives as highly potent antagonists of gastrin/cholecystokinin-B receptors. II

Synthesis of phenoxyacetic acid derivatives as highly potent antagonists of gastrin/cholecystokinin-B receptors. II

  • Chem Pharm Bull (Tokyo). 1998 Jun;46(6):951-61. doi: 10.1248/cpb.46.951.
Y Takeda 1,  K Kawagoe,  A Yokomizo,  Y Yokomizo,  T Hosokami,  Y Shimoto,  Y Tabuchi,  Y Ogihara,  R Otsubo,  Y Honda,  S Yokohama
Affiliations

Affiliation

  • 1 New Product Research Loboratories III, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
PMID: 9658573 DOI: 10.1248/cpb.46.951
Abstract

A series of phenoxyacetanilide derivatives was synthesized and their antagonist activities for human Gastrin/cholecystokinin (CCK)-B and CCK-A receptors were evaluated. Among the compounds synthesized, 2-[3-[3-[N-[2-(N-methyl-N-phenylcarbamoylmethoxy)phenyl]-N-(N-meth yl-N- phenylcarbamoylmethyl)carbamoylmethyl]-ureido]phenyl]acetic acid (20i, DA-3934) exhibited high affinity for Gastrin/CCK-B receptors and high selectivity over CCK-A receptors. DA-3934 and its methyl ester derivative inhibited pentagastrin-induced gastric acid secretion in rats in a dose-dependent manner.

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