Studies on the Synthesis of Cholecystokinin A Receptor Antagonists. III. Synthesis and Cholecystokinin A Receptor Inhibitory Activities of Naphthyl Sulfone Derivatives

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 hydro...

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Veröffentlicht in:	YAKUGAKU ZASSHI 1996/08/25, Vol.116(8), pp.647-656
Hauptverfasser:	AJISAWA, Yukiyoshi, KITAZAWA, Makio, NAKANO, Yasushi, TSUBAKI, Atsushi, BAN, Masaaki, SATO, Kazuaki, OKAZAKI, Kosuke, UCHIDA, Masahiko, KOBAYASHI, Michihiro
Format:	Artikel
Sprache:	eng ; jpn
Schlagworte:	Animals cholecystokinin A receptor antagonist In Vitro Techniques Male Michael addition Naphthalenes - chemical synthesis Naphthalenes - pharmacology naphthyl Rats Rats, Wistar Receptor, Cholecystokinin A Receptors, Cholecystokinin - antagonists & inhibitors Receptors, Cholecystokinin - chemistry Structure-Activity Relationship sulfide sulfone Sulfones - chemical synthesis Sulfones - pharmacology
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Zusammenfassung:	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-naphthylsulfonyl) pentanoic acid ((R)-7c) was selected.
ISSN:	0031-6903 1347-5231
DOI:	10.1248/yakushi1947.116.8_647