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.
Hammerland
Lance G
LG
NPS-Pharmaceuticals, 383 Colorow Drive, Salt Lake City, UT 84108, USA.
Johansson
Martin
M
Malmström
Jonas
J
Mattsson
Jan P
JP
Minidis
Alexander B E
AB
Nilsson
Karolina
K
Peterson
Alecia
A
Wensbo
David
D
Wållberg
Andreas
A
Osterlund
Krister
K
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