Structure-activity relationship of thiopyrimidines as mGluR5 antagonists.
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.
NPS-Pharmaceuticals, 383 Colorow Drive, Salt Lake City, UT 84108, USA.
Lance G
LG
Hammerland
Martin
M
Johansson
Jonas
J
Malmström
Jan P
JP
Mattsson
Alexander B E
AB
Minidis
Karolina
K
Nilsson
Alecia
A
Peterson
David
D
Wensbo
Andreas
A
Wållberg
Krister
K
Osterlund
D000818:Animals; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D006801:Humans; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects; D008861:Microsomes / Q000187:drug effects; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013872:Thionucleosides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
C578935:GRM5 protein, human; C578937:Grm5 protein, rat; D011743:Pyrimidines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; D013872:Thionucleosides