Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
A high-throughput cell-based screen identified a series of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of metabotropic glutamate receptor 5 (mGlu(5)). This Letter describes the SAR of this series and the profile of selected compounds in selectivity and radioligand binding assays.
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Andrew S
AS
Felts
Sam A
SA
Saleh
Uyen
U
Le
Alice L
AL
Rodriguez
C David
CD
Weaver
P Jeffrey
PJ
Conn
Craig W
CW
Lindsley
Kyle A
KA
Emmitte
D000818:Animals; D002460:Cell Line; D015195:Drug Design; D055808:Drug Discovery; D006801:Humans; D015394:Molecular Structure; D011799:Quinazolines / 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
D011799:Quinazolines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate