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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. 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
Inhibition of purified factor Xa amidolytic activity may not be predictive of inhibition of in vivo thrombosis: implications for identification of therapeutically active inhibitors.
Sinha U, Lin PH, Edwards ST, Wong PW, Zhu B, Scarborough RM, Su T, Jia ZJ, Song Y, Zhang P, Clizbe L, Park G, Reed A, Hollenbach SJ, Malinowski J, Arfsten AE. Sinha U, et al. Among authors: jia zj. Arterioscler Thromb Vasc Biol. 2003 Jun 1;23(6):1098-104. doi: 10.1161/01.ATV.0000077248.22632.88. Epub 2003 May 15. Arterioscler Thromb Vasc Biol. 2003. PMID: 12750119
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. 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
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: jia zj. 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: jia zj. 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
222 results