Structure-activity relationship of thiopyrimidines as mGluR5 antagonists

Lance G Hammerland; Martin Johansson; Jonas Malmström; Jan P Mattsson; Alexander B E Minidis; Karolina Nilsson; Alecia Peterson; David Wensbo; Andreas Wållberg; Krister Osterlund

doi:10.1016/j.bmcl.2006.01.100

Structure-activity relationship of thiopyrimidines as mGluR5 antagonists

Bioorg Med Chem Lett. 2006 May 1;16(9):2467-9. doi: 10.1016/j.bmcl.2006.01.100. Epub 2006 Feb 14.

Authors

Lance G Hammerland¹, Martin Johansson, Jonas Malmström, Jan P Mattsson, Alexander B E Minidis, Karolina Nilsson, Alecia Peterson, David Wensbo, Andreas Wållberg, Krister Osterlund

Affiliation

¹ NPS-Pharmaceuticals, 383 Colorow Drive, Salt Lake City, UT 84108, USA.

PMID: 16481165
DOI: 10.1016/j.bmcl.2006.01.100

Abstract

Structure-activity relationship investigations of the thiopyrimidine (1), an HTS hit with micromolar activity as a metabotropic glutamate receptor 5 (mGluR5) antagonist, led to compounds with sub-micromolar activity.

MeSH terms

Animals
Cell Line
Drug Evaluation, Preclinical
Humans
In Vitro Techniques
Liver / drug effects
Microsomes / drug effects
Molecular Structure
Pyrimidines / chemical synthesis
Pyrimidines / chemistry
Pyrimidines / pharmacology*
Rats
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate / antagonists & inhibitors*
Stereoisomerism
Structure-Activity Relationship
Thionucleosides / chemical synthesis
Thionucleosides / chemistry
Thionucleosides / pharmacology*

Substances

GRM5 protein, human
Grm5 protein, rat
Pyrimidines
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate
Thionucleosides