Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
A series of diaryl amides was designed and synthesized as novel nonethynyl mGluR5 antagonists. The systematic variation of the pharmacophoric groups led to the identification of a lead compound that demonstrated micromolar affinity for the mGluR5. Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro.
Kulkarni
Santosh S
SS
Medicinal Chemistry Section, National Institute on Drug Abuse, Intramural Research Program, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
Nightingale
Barbara
B
Dersch
Christina M
CM
Rothman
Richard B
RB
Newman
Amy Hauck
AH