title: Structure based evolution of a novel series of positive modulators of the AMPA receptor.
abstract: Starting from compound 1, we utilized biostructural data to successfully evolve an existing series into a new chemotype with a promising overall profile, exemplified by 19.
authors.affiliation: Merck Research Laboratories, MSD, Newhouse, Motherwell, Lanarkshire ML1 5SH, UK. craig.jamieson@strath.ac.uk
authors.forename: Craig
authors.initials: C
authors.lastname: Jamieson
authors.forename: John K F
authors.initials: JK
authors.lastname: Maclean
authors.forename: Christopher I
authors.initials: CI
authors.lastname: Brown
authors.forename: Robert A
authors.initials: RA
authors.lastname: Campbell
authors.forename: Kevin J
authors.initials: KJ
authors.lastname: Gillen
authors.forename: Jonathan
authors.initials: J
authors.lastname: Gillespie
authors.forename: Bert
authors.initials: B
authors.lastname: Kazemier
authors.forename: Michael
authors.initials: M
authors.lastname: Kiczun
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Lamont
authors.forename: Amanda J
authors.initials: AJ
authors.lastname: Lyons
authors.forename: Elizabeth M
authors.initials: EM
authors.lastname: Moir
authors.forename: John A
authors.initials: JA
authors.lastname: Morrow
authors.forename: John
authors.initials: J
authors.lastname: Pantling
authors.forename: Zoran
authors.initials: Z
authors.lastname: Rankovic
authors.forename: Lynn
authors.initials: L
authors.lastname: Smith
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D002460:Cell Line; D018360:Crystallography, X-Ray; D015195:Drug Design; D006801:Humans; D007189:Indans / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D008862:Microsomes, Liver / Q000378:metabolism; D008958:Models, Molecular; D009422:Nervous System Diseases / Q000188:drug therapy / Q000378:metabolism; D011720:Pyrazoles / Q000737:chemistry / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D018091:Receptors, AMPA / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D007189:Indans; D011720:Pyrazoles; D018091:Receptors, AMPA; D013449:Sulfonamides