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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: song y. 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
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. 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
Design and synthesis of factor Xa inhibitors and their prodrugs.
Song Y, Clizbe L, Bhakta C, Teng W, Wong P, Huang B, Tran K, Sinha U, Park G, Reed A, Scarborough RM, Zhu BY. Song Y, et al. Bioorg Med Chem Lett. 2003 Jan 20;13(2):297-300. doi: 10.1016/s0960-894x(02)00921-6. Bioorg Med Chem Lett. 2003. PMID: 12482444
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: song y. 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: song y. 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: song y. 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: song y. 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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