| Literature DB >> 12565972 |
Wenrong Huang1, Penglie Zhang, Jingmei F Zuckett, Lingyan Wang, John Woolfrey, Yonghong Song, Zhaozhong J Jia, Lane A Clizbe, Ting Su, Katherine Tran, Brian Huang, Paul Wong, Uma Sinha, Gary Park, Andrea Reed, John Malinowski, Stanley J Hollenbach, Robert M Scarborough, Bing-Yan Zhu.
Abstract
A series of benzoxazinone derivatives was designed and synthesized as factor Xa inhibitors. We demonstrated that the naphthyl moiety in the aniline-based compounds 1 and 2 can be replaced with benzene-fused heterobicycles and biaryls to give factor Xa inhibitors with improved trypsin selectivity. The P4 modifications lead to monoamidines which are moderately active. The benzoxazinones 41-45 are potent against factor Xa, retain the improved trypsin selectivity of the corresponding aniline-based compounds, and show strong antithrombotic effect dose responsively.Entities:
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Year: 2003 PMID： 12565972 DOI： 10.1016/s0960-894x(02)00927-7
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823