Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.
We described the synthesis and biological evaluation of MPEP analogs functionalized at the position 3 of the phenyl ring. The results point out the limitation in the choice of a functional group at this position; the only substituents leading to retention of activity are NO(2) (IC(50)=13 nM) and CN (IC(50)=8 nM).
Alagille
David
D
Department of Psychiatry, Yale University and VA Connecticut/116A2, 950 Campbell Avenue, West Haven, CT 06516, USA.
Baldwin
Ronald M
RM
Roth
Bryan L
BL
Wroblewski
Jarda T
JT
Grajkowska
Ewa
E
Tamagnan
Gilles D
GD
D000818:Animals; D020128:Inhibitory Concentration 50; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018092:Kainic Acid Receptors / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D011725:Pyridines; D018092:Kainic Acid Receptors; C121465:6-methyl-2-(phenylethynyl)pyridine