Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.
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.
Lee
K
K
Biotech Research Institute, LG Chemical Ltd/Research Park, Science Town, Taejon, Korea.
Jung
W H
WH
Hwang
S Y
SY
Lee
S H
SH
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
D000991:Antithrombins; D001549:Benzamides; D005461:Fluorine