title: Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
abstract: LB30057 (1) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound 1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity. Compound 2 demonstrated a 3-fold increase in absorption.
authors.affiliation: Biotech Research Institute, LG Chemical Ltd/Research Park, Science Town, Taejon, Korea.
authors.forename: K
authors.initials: K
authors.lastname: Lee
authors.forename: W H
authors.initials: WH
authors.lastname: Jung
authors.forename: S Y
authors.initials: SY
authors.lastname: Hwang
authors.forename: S H
authors.initials: SH
authors.lastname: Lee
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000991:Antithrombins / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001549:Benzamides / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004285:Dogs; D005461:Fluorine / Q000737:chemistry*; D051381:Rats
chemical_list: D000991:Antithrombins; D001549:Benzamides; D005461:Fluorine