title: Discovery of novel modulators of metabotropic glutamate receptor subtype-5.
abstract: A series of potent and selective mGluR5 antagonists were synthesized and evaluated in vitro and in vivo. It was found that a pyridyl functionality is a potential replacement for acetonitrile in the lead structure, with 2-pyridyl being most favored. Additionally, the benzoxazole moiety could also be replaced by other heterobicyclic rings such as imidazothiazole.
authors.affiliation: Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, 92121, San Diego, CA 92121, USA. bowei_wang@merck.com
authors.forename: Bowei
authors.initials: B
authors.lastname: Wang
authors.forename: Jean Michel
authors.initials: JM
authors.lastname: Vernier
authors.forename: Sara
authors.initials: S
authors.lastname: Rao
authors.forename: Janice
authors.initials: J
authors.lastname: Chung
authors.forename: Jeffery J
authors.initials: JJ
authors.lastname: Anderson
authors.forename: Jesse D
authors.initials: JD
authors.lastname: Brodkin
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Jiang
authors.forename: Michael F
authors.initials: MF
authors.lastname: Gardner
authors.forename: Xiaoqing
authors.initials: X
authors.lastname: Yang
authors.forename: Benito
authors.initials: B
authors.lastname: Munoz
mesh_terms: D000818:Animals; D001583:Benzoxazoles / Q000737:chemistry / Q000494:pharmacology*; D001682:Biological Availability; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000502:physiology
chemical_list: D001583:Benzoxazoles; D018691:Excitatory Amino Acid Antagonists; C578937:Grm5 protein, rat; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate