Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP

被引：29

作者：

Alagille, D

Baldwin, RM

Roth, BL

Wroblewski, JT

Grajkowska, E

Tamagnan, GD

机构：

[1] Yale Univ, Dept Psychiat, West Haven, CT 06516 USA

[2] VA Connecticut 116A2, West Haven, CT 06516 USA

[3] Case Western Reserve Univ, Sch Med, Dept Biochem, Cleveland, OH 44106 USA

[4] Case Western Reserve Univ, Sch Med, NIMH, Psychoact Drug Screening Program, Cleveland, OH 44106 USA

[5] Georgetown Univ, Med Ctr, Dept Pharmacol, Washington, DC 20007 USA

[6] Inst Neurodegenerat Disorders, New Haven, CT 06510 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 04期

关键词：

metabotropic; mGluR5; MPEP; antagonist;

D O I：

10.1016/j.bmcl.2004.12.047

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We described the synthesis and biological evaluation of MPEP analogs functionalized at the position 3 of the phenyl ring. The results point out the limitation in the choice of a functional group at this position; the only substituents leading to retention of activity are NO2 (IC50 = 13 nM) and CN (IC50 = 8 nM). (C) 2004 Elsevier Ltd. All rights reserved.

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页码：945 / 949

页数：5

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