62686-69-5Relevant academic research and scientific papers
Structural modification of an orally active thrombin inhibitor, LB30057: Replacement of the D-pocket-binding naphthyl moiety
Lee, Koo,Hwang, Sang Yeul,Hong, Seongwon,Hong, Chang Yong,Lee, Chang-Seok,Shin, Youseung,Kim, Sangsoo,Yun, Mikyung,Yoo, Yung Joon,Kang, Myunggyun,Oh, Yeong Soo
, p. 869 - 876 (1998)
An amidrazonophenylalanine derivative LB30057 (2) was identified as a potent (K(i)=0.38nM), selective, and orally active thrombin inhibitor. As a continuation of studies into benzamidrazone-based thrombin inhibitors, we have structurally modified compound 2 by replacing the naphthyl group with a variety of hydrophobic moieties. This study led to discovery of several compounds with significantly enhanced potency in thrombin inhibition without sacrificing selectivity against trypsin and oral absorption. The highest activity was obtained with compound 23 (K(i)=0.045nM). Copyright (C) 1998 Elsevier Science Ltd.
