Novel 3,4,7-Substituted Benzofuran Derivatives Having Binding Affinity to [kappa]-Opioid Receptor

A series of novel 3,4,7-trisubstituted benzofuran derivatives were synthesized, and their binding affinity to [kappa]- (KOR) and μ-opioid receptors (MOR) were evaluated. Several aryl ethers showed moderate binding activities to KOR (IC50=3.9-11 µM) without binding to MOR.

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Veröffentlicht in:Chemical & pharmaceutical bulletin 2016-07, Vol.64 (7), p.996
Hauptverfasser: Nishiyama, Daisuke, Sakai, Yuki, Sekiguchi, Haruka, Chiba, Hiroaki, Misu, Ryosuke, Oishi, Shinya, Fujii, Nobutaka, Ohno, Hiroaki
Format: Artikel
Sprache:eng
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Zusammenfassung:A series of novel 3,4,7-trisubstituted benzofuran derivatives were synthesized, and their binding affinity to [kappa]- (KOR) and μ-opioid receptors (MOR) were evaluated. Several aryl ethers showed moderate binding activities to KOR (IC50=3.9-11 µM) without binding to MOR.
ISSN:0009-2363
1347-5223