Title of article :
Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity
Author/Authors :
NICHOLAS D. SMITH & ANDREW C. YIP، نويسنده , , Steve F. Poon، نويسنده , , Dehua Huang، نويسنده , , Mitchell Green، نويسنده , , R. Christopher King MD، نويسنده , , Lida Tehrani، نويسنده , , Jeffrey R. Roppe، نويسنده , , Janice Chung، نويسنده , , Deborah P. Chapman، نويسنده , , Merryl Cramer، نويسنده , , Nicholas D.P Cosford، نويسنده ,
Abstract :
Structure–activity relationship studies focused on bio-isosteric replacements of 2-pyridyl resulted in mGlu5 receptor antagonists with reduced inhibition of cytochrome P450 1A2. This led to highly potent, selective and orally bioavailable 2-imidazolyl tetrazoles such as (10) that are devoid of cytochrome P450 inhibitory activity.
Keywords :
Metabotropic glutamate , Antagonist , tetrazole , CytochromeP450 1A2.
