title: Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists.
abstract: 1H-pyrrolo[2,3-c]pyridine-7-carboxamides constitute a new series of allosteric mGluR5 antagonists. Variation of the substituents attached to the heterocyclic scaffold allowed to improve the physico-chemical parameters for optimization of the aqueous solubility while retaining high in vitro potency.
authors.affiliation: Novartis Institutes for BioMedical Research, Global Discovery Chemistry, 4002 Basel, Switzerland. koller_manuel@bluewin.ch
authors.forename: Manuel
authors.initials: M
authors.lastname: Koller
authors.forename: David A
authors.initials: DA
authors.lastname: Carcache
authors.forename: David
authors.initials: D
authors.lastname: Orain
authors.forename: Peter
authors.initials: P
authors.lastname: Ertl
authors.forename: Dirk
authors.initials: D
authors.lastname: Behnke
authors.forename: Sandrine
authors.initials: S
authors.lastname: Desrayaud
authors.forename: Grit
authors.initials: G
authors.lastname: Laue
authors.forename: Ivo
authors.initials: I
authors.lastname: Vranesic
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000577:Amides / Q000737:chemistry* / Q000494:pharmacology*; D055808:Drug Discovery; D006801:Humans; D020128:Inhibitory Concentration 50; D011728:Pyridones / Q000737:chemistry* / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012995:Solubility
chemical_list: D000577:Amides; C578935:GRM5 protein, human; D011728:Pyridones; D011758:Pyrroles; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate