title: Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies.
abstract: Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
authors.affiliation: AstraZeneca, Alderley Park, Macclesfield, Cheshire, SK10 4TG, UK. paul.whittamore@astrazeneca.com
authors.forename: Paul R O
authors.initials: PR
authors.lastname: Whittamore
authors.forename: Matthew S
authors.initials: MS
authors.lastname: Addie
authors.forename: Stuart N L
authors.initials: SN
authors.lastname: Bennett
authors.forename: Alan M
authors.initials: AM
authors.lastname: Birch
authors.forename: Michael
authors.initials: M
authors.lastname: Butters
authors.forename: Linda
authors.initials: L
authors.lastname: Godfrey
authors.forename: Peter W
authors.initials: PW
authors.lastname: Kenny
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Morley
authors.forename: Paul M
authors.initials: PM
authors.lastname: Murray
authors.forename: Nikos G
authors.initials: NG
authors.lastname: Oikonomakos
authors.forename: Ludovic R
authors.initials: LR
authors.lastname: Otterbein
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Pannifer
authors.forename: Jeremy S
authors.initials: JS
authors.lastname: Parker
authors.forename: Kristy
authors.initials: K
authors.lastname: Readman
authors.forename: Pawel S
authors.initials: PS
authors.lastname: Siedlecki
authors.forename: Paul
authors.initials: P
authors.lastname: Schofield
authors.forename: Andy
authors.initials: A
authors.lastname: Stocker
authors.forename: Melvyn J
authors.initials: MJ
authors.lastname: Taylor
authors.forename: Linda A
authors.initials: LA
authors.lastname: Townsend
authors.forename: David P
authors.initials: DP
authors.lastname: Whalley
authors.forename: Jennifer
authors.initials: J
authors.lastname: Whitehouse
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors*; D006801:Humans; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D011758:Pyrroles; D024981:Glycogen Phosphorylase