Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Peter Bach; Karolina Nilsson; Tor Svensson; Udo Bauer; Lance G Hammerland; Alecia Peterson; Andreas Wållberg; Krister Osterlund; David Karis; Maria Boije; David Wensbo

doi:10.1016/j.bmcl.2006.06.078

Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4788-91. doi: 10.1016/j.bmcl.2006.06.078. Epub 2006 Jul 11.

Authors

Peter Bach¹, Karolina Nilsson, Tor Svensson, Udo Bauer, Lance G Hammerland, Alecia Peterson, Andreas Wållberg, Krister Osterlund, David Karis, Maria Boije, David Wensbo

Affiliation

¹ Department of Medicinal Chemistry, AstraZeneca R&D Mölndal, Pepparedsleden 1, S-431 83 Mölndal, Sweden. [email protected]

PMID: 16837196
DOI: 10.1016/j.bmcl.2006.06.078

Abstract

Studies of structure-activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data.

MeSH terms

Alkynes / chemical synthesis
Alkynes / chemistry*
Alkynes / pharmacokinetics
Alkynes / pharmacology*
Animals
Cross-Linking Reagents / chemistry*
Liver / drug effects
Liver / metabolism
Molecular Structure
Pyridines / chemistry*
Rats
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate / antagonists & inhibitors*
Receptors, Metabotropic Glutamate / metabolism*
Structure-Activity Relationship

Substances

Alkynes
Cross-Linking Reagents
Grm5 protein, rat
Pyridines
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate
pyridine