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.
Felts
Andrew S
AS
Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Saleh
Sam A
SA
Le
Uyen
U
Rodriguez
Alice L
AL
Weaver
C David
CD
Conn
P Jeffrey
PJ
Lindsley
Craig W
CW
Emmitte
Kyle A
KA
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