title: Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.
abstract: Imidazo[1,2-a]pyridines were identified via their shape and electrostatic similarity as novel positive allosteric modulators of the metabotropic glutamate 2 receptor. The subsequent synthesis and SAR are described. Potent, selective and metabolically stable compounds were found representing a promising avenue for current further studies.
authors.affiliation: Research Informatics, Johnson & Johnson, Pharmaceutical Research & Development, Janssen-Cilag S.A., Calle Jarama 75, Poligono Industrial, Toledo 45007, Spain. gtresade@its.jnj.com
authors.forename: Gary
authors.initials: G
authors.lastname: Tresadern
authors.forename: Jose María
authors.initials: JM
authors.lastname: Cid
authors.forename: Gregor J
authors.initials: GJ
authors.lastname: Macdonald
authors.forename: Juan Antonio
authors.initials: JA
authors.lastname: Vega
authors.forename: Ana Isabel
authors.initials: AI
authors.lastname: de Lucas
authors.forename: Aránzazu
authors.initials: A
authors.lastname: García
authors.forename: Encarnación
authors.initials: E
authors.lastname: Matesanz
authors.forename: María Lourdes
authors.initials: ML
authors.lastname: Linares
authors.forename: Daniel
authors.initials: D
authors.lastname: Oehlrich
authors.forename: Hilde
authors.initials: H
authors.lastname: Lavreysen
authors.forename: Ilse
authors.initials: I
authors.lastname: Biesmans
authors.forename: Andrés A
authors.initials: AA
authors.lastname: Trabanco
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D006801:Humans; D007093:Imidazoles / Q000737:chemistry*; D008862:Microsomes, Liver / Q000378:metabolism; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011728:Pyridones / Q000737:chemistry*; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000737:chemistry* / Q000378:metabolism; D055672:Static Electricity; D013329:Structure-Activity Relationship
chemical_list: D007093:Imidazoles; D011725:Pyridines; D011728:Pyridones; D018094:Receptors, Metabotropic Glutamate; C108822:metabotropic glutamate receptor 2; C029899:imidazole