Chemical and Pharmaceutical Bulletin p. 434 - 444 (1998)
Update date:2022-07-30
Topics:
Takeda, Yasuyuki
Kawagoe, Keiichi
Yokomizo, Aki
Yokomizo, Yoshihiro
Hosokami, Toru
Ogihara, Yoshiyasu
Honda, Yuko
Yokohama, Shuichi
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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