title: Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. Part 6: further focus on the contracted C4'-side chain analogues.
abstract: Novel benzo[b]thiophene diamine thrombin inhibitors were investigated, focusing on a contracted C4'-side chain series. SAR studies identified compounds with either a pyrrolidino or morpholino group as potent, active site directed thrombin inhibitors when the amino group was connected to the C3-phenyl ring with a methylene linker at the C4' position of the phenyl ring.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. ktak@lilly.com
authors.forename: K
authors.initials: K
authors.lastname: Takeuchi
authors.forename: T J
authors.initials: TJ
authors.lastname: Kohn
authors.forename: R W
authors.initials: RW
authors.lastname: Harper
authors.forename: H S
authors.initials: HS
authors.lastname: Lin
authors.forename: D S
authors.initials: DS
authors.lastname: Gifford-Moore
authors.forename: M E
authors.initials: ME
authors.lastname: Richett
authors.forename: D J
authors.initials: DJ
authors.lastname: Sall
authors.forename: G F
authors.initials: GF
authors.lastname: Smith
authors.forename: M
authors.initials: M
authors.lastname: Zhang
mesh_terms: D000991:Antithrombins / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000991:Antithrombins; D013876:Thiophenes; C088015:benzothiophene