title: Discovery of LB30057, a benzamidrazone-based selective oral thrombin inhibitor.
abstract: Systematic variation of the so-called P-pocket moiety of benzamidrazone-based selective thrombin inhibitors led to the discovery of LB30057. It is potent (Ki = 0.38 nM for human thrombin), selective (Ki = 3290 nM for bovine trypsin), and orally bioavailable (58% oral bioavailability in dogs). LB30057 was efficacious in thrombosis animal models.
authors.affiliation: Biotech Research Institute, LG Chemical LTD, Taejon, Korea.
authors.forename: Y S
authors.initials: YS
authors.lastname: Oh
authors.forename: M
authors.initials: M
authors.lastname: Yun
authors.forename: S Y
authors.initials: SY
authors.lastname: Hwang
authors.forename: S
authors.initials: S
authors.lastname: Hong
authors.forename: Y
authors.initials: Y
authors.lastname: Shin
authors.forename: K
authors.initials: K
authors.lastname: Lee
authors.forename: K H
authors.initials: KH
authors.lastname: Yoon
authors.forename: Y J
authors.initials: YJ
authors.lastname: Yoo
authors.forename: D S
authors.initials: DS
authors.lastname: Kim
authors.forename: S H
authors.initials: SH
authors.lastname: Lee
authors.forename: Y H
authors.initials: YH
authors.lastname: Lee
authors.forename: H D
authors.initials: HD
authors.lastname: Park
authors.forename: C H
authors.initials: CH
authors.lastname: Lee
authors.forename: S K
authors.initials: SK
authors.lastname: Lee
authors.forename: S
authors.initials: S
authors.lastname: Kim
mesh_terms: D000818:Animals; D001549:Benzamides / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D001682:Biological Availability; D002417:Cattle; D004195:Disease Models, Animal; D004285:Dogs; D006207:Half-Life; D006801:Humans; D008958:Models, Molecular; D051381:Rats; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors*; D013927:Thrombosis / Q000188:drug therapy
chemical_list: D001549:Benzamides; C116605:LB 30057; D013917:Thrombin