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44 results
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Page 1
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.
Isaacs RC, Newton CL, Cutrona KJ, Mercer SP, Payne LS, Stauffer KJ, Williams PD, Cook JJ, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Lynch JJ, McMasters DR, Naylor-Olsen AM, Michener MT, Wallace AA. Isaacs RC, et al. Among authors: krueger ja. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1536-40. doi: 10.1016/j.bmcl.2010.12.105. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21295467
P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.
Isaacs RC, Newton CL, Cutrona KJ, Mercer SP, Dorsey BD, McDonough CM, Cook JJ, Krueger JA, Lewis SD, Lucas BJ, Lyle EA, Lynch JJ, Miller-Stein C, Michener MT, Wallace AA, White RB, Wong BK. Isaacs RC, et al. Among authors: krueger ja. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1532-5. doi: 10.1016/j.bmcl.2010.12.108. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21295466
The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model.
Rossman EI, Liu K, Morgan GA, Swillo RE, Krueger JA, Gardell SJ, Butera J, Gruver M, Kantrowitz J, Feldman HS, Petersen JS, Haugan K, Hennan JK. Rossman EI, et al. Among authors: krueger ja. J Pharmacol Exp Ther. 2009 Jun;329(3):1127-33. doi: 10.1124/jpet.108.150102. Epub 2009 Feb 27. J Pharmacol Exp Ther. 2009. PMID: 19252062
A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia.
Evans MJ, Mahaney PE, Borges-Marcucci L, Lai K, Wang S, Krueger JA, Gardell SJ, Huard C, Martinez R, Vlasuk GP, Harnish DC. Evans MJ, et al. Among authors: krueger ja. Am J Physiol Gastrointest Liver Physiol. 2009 Mar;296(3):G543-52. doi: 10.1152/ajpgi.90585.2008. Epub 2009 Jan 8. Am J Physiol Gastrointest Liver Physiol. 2009. PMID: 19136377 Free article.
Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 2: N-acetamidoimidazoles.
Isaacs RC, Solinsky MG, Cutrona KJ, Newton CL, Naylor-Olsen AM, McMasters DR, Krueger JA, Lewis SD, Lucas BJ, Kuo LC, Yan Y, Lynch JJ, Lyle EA. Isaacs RC, et al. Among authors: krueger ja. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2062-6. doi: 10.1016/j.bmcl.2008.01.098. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18291642
44 results