N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.
作者信息
Jia Zhaozhong J, Su Ting, Zuckett Jingmei F, Wu Yanhong, Goldman Erick A, Li Wenhao, Zhang Penglie, Clizbe Lane A, Song Yonghong, Bauer Shawn M, Huang Wenrong, Woolfrey John, Sinha Uma, Arfsten Ann E, Hutchaleelaha Athiwat, Hollenbach Stanley J, Lambing Joseph L, Scarborough Robert M, Zhu Bing-Yan
机构信息
Millennium Pharmaceuticals, Inc., 256 East Grand Ave, South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2004 May 3;14(9):2073-8. doi: 10.1016/j.bmcl.2004.02.049.
A class of N,N-dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines has been discovered as potent factor Xa inhibitors with desirable in vitro and in vivo anticoagulant activity, but with low oral bioavailability. The 5-chloroindole and 6-chlorobenzo[b]thiophene groups are optimal as the factor Xa S1 binding elements. The strategy of incorporating a side chain on the piperazine nucleus to enhance binding affinity has been examined.
Zotero 插件