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Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.
Jia ZJ, Wu Y, Huang W, Goldman E, Zhang P, Woolfrey J, Wong P, Huang B, Sinha U, Park G, Reed A, Scarborough RM, Zhu BY. Jia ZJ, et al. Among authors: huang b, huang w. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1651-5. doi: 10.1016/s0960-894x(02)00239-1. Bioorg Med Chem Lett. 2002. PMID: 12039583
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
Jia ZJ, Wu Y, Huang W, Zhang P, Song Y, Woolfrey J, Sinha U, Arfsten AE, Edwards ST, Hutchaleelaha A, Hollennbach SJ, Lambing JL, Scarborough RM, Zhu BY. Jia ZJ, et al. Among authors: huang w. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1229-34. doi: 10.1016/j.bmcl.2003.12.054. Bioorg Med Chem Lett. 2004. PMID: 14980671
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: huang 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
Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors.
Bauer SM, Goldman EA, Huang W, Su T, Wang L, Woolfrey J, Wu Y, Zuckett JF, Arfsten A, Huang B, Kothule J, Lin J, May B, Sinha U, Wong PW, Hutchaleelaha A, Scarborough RM, Zhu BY. Bauer SM, et al. Among authors: huang b, huang w. Bioorg Med Chem Lett. 2004 Aug 2;14(15):4045-50. doi: 10.1016/j.bmcl.2004.05.033. Bioorg Med Chem Lett. 2004. PMID: 15225723
Inhibitory effect of carboxylic acid group on hERG binding.
Zhu BY, Jia ZJ, Zhang P, Su T, Huang W, Goldman E, Tumas D, Kadambi V, Eddy P, Sinha U, Scarborough RM, Song Y. Zhu BY, et al. Among authors: huang w. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5507-12. doi: 10.1016/j.bmcl.2006.08.039. Epub 2006 Aug 22. Bioorg Med Chem Lett. 2006. PMID: 16931010
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: huang 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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