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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: clizbe l. 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. Among authors: clizbe la. 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: clizbe l. 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. Among authors: clizbe l. 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
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: clizbe la. 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