Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption

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. Compoun...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 1999-09, Vol.9 (17), p.2483-2486
Hauptverfasser: Lee, Koo, Jung, Won-Hyuk, Hwang, Sang Yeul, Lee, Sung-Hack
Format: Artikel
Sprache:eng
Schlagworte:
Administration, Oral
Animals
Antithrombins - administration & dosage
Antithrombins - chemistry
Antithrombins - pharmacokinetics
Benzamides - administration & dosage
Benzamides - chemistry
Benzamides - pharmacokinetics
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Dogs
Fluorine - chemistry
Medical sciences
Pharmacology. Drug treatments
Rats
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Zusammenfassung: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00412-6