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苯氧乙酸衍生物作为胃泌素/胆囊收缩素-B受体高效拮抗剂的合成。II.

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

作者信息

Takeda Y, Kawagoe K, Yokomizo A, Yokomizo Y, Hosokami T, Shimoto Y, Tabuchi Y, Ogihara Y, Otsubo R, Honda Y, Yokohama S

机构信息

New Product Research Loboratories III, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1998 Jun;46(6):951-61. doi: 10.1248/cpb.46.951.

DOI:10.1248/cpb.46.951
PMID:9658573
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.

摘要

合成了一系列苯氧乙酰胺衍生物，并评估了它们对人胃泌素/胆囊收缩素（CCK）-B和CCK-A受体的拮抗活性。在合成的化合物中，2-[3-[3-[N-[2-(N-甲基-N-苯基氨基甲酰基甲氧基)phenyl]-N-(N-甲基-N-苯基氨基甲酰基甲基)氨基甲酰基甲基]-脲基]phenyl]乙酸（20i，DA-3934）对胃泌素/CCK-B受体表现出高亲和力，对CCK-A受体具有高选择性。DA-3934及其甲酯衍生物以剂量依赖方式抑制大鼠中五肽胃泌素诱导的胃酸分泌。

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