Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption

K Lee, WH Jung, SY Hwang, SH Lee

文献索引：Lee, Koo; Jung, Won-Hyuk; Sang, Yeul Hwang; Lee, Sung-Hack Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 17 p. 2483 - 2486

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被引用次数: 17

摘要

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.