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N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors.
Jia ZJ, Su T, Zuckett JF, Wu Y, Goldman EA, Li W, Zhang P, Clizbe LA, Song Y, Bauer SM, Huang W, Woolfrey J, Sinha U, Arfsten AE, Hutchaleelaha A, Hollenbach SJ, Lambing JL, Scarborough RM, Zhu BY. Jia ZJ, et al. Among authors: li w. Bioorg Med Chem Lett. 2004 May 3;14(9):2073-8. doi: 10.1016/j.bmcl.2004.02.049. Bioorg Med Chem Lett. 2004. PMID: 15080981
Design, synthesis, and SAR of substituted acrylamides as factor Xa inhibitors.
Song Y, Clizbe L, Bhakta C, Teng W, Li W, Wu Y, Jia ZJ, Zhang P, Wang L, Doughan B, Su T, Kanter J, Woolfrey J, Wong P, Huang B, Tran K, Sinha U, Park G, Reed A, Malinowski J, Hollenbach S, Scarborough RM, Zhu BY. Song Y, et al. Among authors: li w. Bioorg Med Chem Lett. 2002 Jun 3;12(11):1511-5. doi: 10.1016/s0960-894x(02)00199-3. Bioorg Med Chem Lett. 2002. PMID: 12031331
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.
Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. Zhang P, et al. Among authors: li w. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85. doi: 10.1016/j.bmcl.2009.02.111. Epub 2009 Mar 3. Bioorg Med Chem Lett. 2009. PMID: 19297154
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