2. Academic Validation
  3. [Studies on the synthesis of cholecystokinin A receptor antagonists. III. Synthesis and cholecystokinin A receptor inhibitory activities of naphthyl sulfone derivatives]

[Studies on the synthesis of cholecystokinin A receptor antagonists. III. Synthesis and cholecystokinin A receptor inhibitory activities of naphthyl sulfone derivatives]

  • Yakugaku Zasshi. 1996 Aug;116(8):647-56. doi: 10.1248/yakushi1947.116.8_647.
Y Ajisawa 1,  M Kitazawa,  Y Nakano,  A Tsubaki,  M Ban,  K Sato,  K Okazaki,  M Uchida,  M Kobayashi
Affiliations

Affiliation

  • 1 Central Research Laboratories, Kissei Pharmaceutical Co., Ltd., Nagano, Japan.
PMID: 8831266 DOI: 10.1248/yakushi1947.116.8_647
Abstract

A number of naphthyl sulfone derivatives were synthesized and tested for cholecystokinin A (CCK-A) receptor inhibitory activity in order to study structure-activity relationships. Significant CCK-A receptor inhibitory activities were found in sulfone-carboxylic acid derivatives (7) having very hydrophobic sidechains. As the most preferred compound, (R)-4-[N-(3-methoxypropyl)-N-pentylcarbamoyl]-5-(2-naphthylsulf onyl) pentanoic acid ((R)-7c) was selected.

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