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

DOI: 10.1248/cpb.46.434

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 434 - 444 (1998)

Update date:2022-07-30

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Authors:

Takeda, YasuyukiTakeda, Yasuyuki

Kawagoe, KeiichiKawagoe, Keiichi

Yokomizo, AkiYokomizo, Aki

Yokomizo, YoshihiroYokomizo, Yoshihiro

Hosokami, ToruHosokami, Toru

Ogihara, YoshiyasuOgihara, Yoshiyasu

Honda, YukoHonda, Yuko

Yokohama, ShuichiYokohama, Shuichi

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Article abstract of DOI:10.1248/cpb.46.434

A novel series of phenoxyacetic acid derivatives was synthesized based on considerations of the three-dimensional structural similarity of YM022 and RP72540. The gastrin/cholecystokinin (CCK)-B and CCK-A receptor antagonist activities of these compounds were evaluated by investigation of their affinities for human gastrin/CCK-B receptors and human CCK-A receptors, respectively. It was found that N-methyl-N-phenyl-2-[2-[N-(N-methyl-N- phenyl-carbamoylmethyl)-N-[2-[3-(3- methylphenyl)ureido]acetyl]amino]phenoxy]acetamide (20k, DZ-3514) exhibited high affinity for gastrin/CCK-B receptors and high selectivity over CCK-A receptors.

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Full text of DOI:10.1248/cpb.46.434

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Products guided by the article

Product name:Carbamic acid, [2-oxo-2-[[2-(phenylmethoxy)phenyl]amino]ethyl]-, 1,1-dimethylethyl ester

Cas No:183180-09-8

183180-09-8

R&D Labs maybe for 183180-09-8

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