Bioorganic and Medicinal Chemistry Letters p. 2483 - 2486 (1999)
Update date:2022-08-04
Topics: In vitro in vivo Pharmacokinetics Fluorine Thrombin inhibitors
Lee, Koo
Jung, Won-Hyuk
Sang, Yeul Hwang
Lee, Sung-Hack
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.
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