Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

TY - JOUR

T1 - Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4)

AU - Williams, Richard

AU - Johnson, Kari A

AU - Gentry, Patrick R

AU - Niswender, Colleen M

AU - Weaver, Charles D

AU - Conn, P Jeffrey

AU - Lindsley, Craig W

AU - Hopkins, Corey R

PY - 2009/9/1

Y1 - 2009/9/1

N2 - This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease. The synthesis takes advantage of an iterative parallel synthesis approach to rapidly synthesize and evaluate a number of analogs of VU0155041.

AB - This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease. The synthesis takes advantage of an iterative parallel synthesis approach to rapidly synthesize and evaluate a number of analogs of VU0155041.

KW - Allosteric Regulation/drug effects

KW - Allosteric Site

KW - Anilides/chemical synthesis

KW - Animals

KW - Cyclohexanecarboxylic Acids/chemical synthesis

KW - Disease Models, Animal

KW - Parkinson Disease/drug therapy

KW - Rats

KW - Receptors, Metabotropic Glutamate/chemistry

KW - Structure-Activity Relationship

U2 - 10.1016/j.bmcl.2009.07.072

DO - 10.1016/j.bmcl.2009.07.072

M3 - Journal article

C2 - 19640716

SN - 0960-894X

VL - 19

SP - 4967

EP - 4970

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 17

ER -