title: Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
abstract: 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.
authors: Medicinal Chemistry Section, National Institute on Drug Abuse, Intramural Research Program, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
authors: Santosh S
authors: SS
authors: Kulkarni
authors: Barbara
authors: B
authors: Nightingale
authors: Christina M
authors: CM
authors: Dersch
authors: Richard B
authors: RB
authors: Rothman
authors: Amy Hauck
authors: AH
authors: Newman