Discovery of novel triazole-based opioid receptor antagonists

被引：26

作者：

Zhang, Qiang

Keenan, Susan M.

Peng, Youyi

Nair, Anil C.

Yu, Seong Jae

Howells, Richard D.

Welsh, William J. ^{[1
]}

机构：

[1] Univ Med & Dent New Jersey, Robert Wood Johnson Med Sch, Dept Pharmacol, Piscataway, NJ 08854 USA

[2] Univ Med & Dent New Jersey, Inst Informat, Piscataway, NJ 08854 USA

[3] Univ Missouri, Dept Chem & Biochem, St Louis, MO 63121 USA

[4] Univ Med & Dent New Jersey, New Jersey Med Sch, Dept Biochem & Mol Biol, Newark, NJ 07101 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 14期

关键词：

D O I：

10.1021/jm0601250

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the computer-aided design, chemical synthesis, and biological evaluation of a novel family of delta opioid receptor (DOR) antagonists containing a 1,2,4-triazole core structure that are structurally distinct from other known opioid receptor active ligands. Among those delta antagonists sharing this core structure, 8 exhibited strong binding affinity (K-i = 50 nM) for the DOR and appreciable selectivity for delta over mu and kappa opioid receptors (delta/mu = 80; delta/kappa > 200).

引用

收藏

页码：4044 / 4047

页数：4

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