Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5.
Kulkarni
Santosh S
SS
Medicinal Chemistry Section, National Institute on Drug Abuse, Intramural Research Program, NIH, DHHS, Baltimore, MD 21224, USA.
Newman
Amy Hauck
AH
D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D006868:Hydrolysis; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology
C472365:3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine; D019086:Bridged Bicyclo Compounds, Heterocyclic; C578935:GRM5 protein, human; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; D013844:Thiazoles; C121465:6-methyl-2-(phenylethynyl)pyridine