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Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
Murugesan N, Tellew JE, Gu Z, Kunst BL, Fadnis L, Cornelius LA, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Panchal B, Valentine MT, Chong S, Morrison RA, Carlson KE, Powell JR, Moreland S, Barrish JC, Kowala MC, Macor JE. Murugesan N, et al. Among authors: yang y. J Med Chem. 2002 Aug 29;45(18):3829-35. doi: 10.1021/jm020138n. J Med Chem. 2002. PMID: 12190306
Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.
Murugesan N, Gu Z, Fadnis L, Tellew JE, Baska RA, Yang Y, Beyer SM, Monshizadegan H, Dickinson KE, Valentine MT, Humphreys WG, Lan SJ, Ewing WR, Carlson KE, Kowala MC, Zahler R, Macor JE. Murugesan N, et al. Among authors: yang y. J Med Chem. 2005 Jan 13;48(1):171-9. doi: 10.1021/jm049548x. J Med Chem. 2005. PMID: 15634011
Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series.
Ellsworth BA, Wang Y, Zhu Y, Pendri A, Gerritz SW, Sun C, Carlson KE, Kang L, Baska RA, Yang Y, Huang Q, Burford NT, Cullen MJ, Johnghar S, Behnia K, Pelleymounter MA, Washburn WN, Ewing WR. Ellsworth BA, et al. Among authors: yang y. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3978-82. doi: 10.1016/j.bmcl.2007.04.087. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17513109
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.
Ellsworth BA, Sher PM, Wu X, Wu G, Sulsky RB, Gu Z, Murugesan N, Zhu Y, Yu G, Sitkoff DF, Carlson KE, Kang L, Yang Y, Lee N, Baska RA, Keim WJ, Cullen MJ, Azzara AV, Zuvich E, Thomas MA, Rohrbach KW, Devenny JJ, Godonis HE, Harvey SJ, Murphy BJ, Everlof GG, Stetsko PI, Gudmundsson O, Johnghar S, Ranasinghe A, Behnia K, Pelleymounter MA, Ewing WR. Ellsworth BA, et al. Among authors: yang y. J Med Chem. 2013 Dec 12;56(23):9586-600. doi: 10.1021/jm4010835. Epub 2013 Nov 20. J Med Chem. 2013. PMID: 24182233
Novel dual action AT1 and ETA receptor antagonists reduce blood pressure in experimental hypertension.
Kowala MC, Murugesan N, Tellew J, Carlson K, Monshizadegan H, Ryan C, Gu Z, Kane B, Fadnis L, Baska RA, Beyer S, Arthur S, Dickinson K, Zhang D, Perrone M, Ferrer P, Giancarli M, Baumann J, Bird E, Panchal B, Yang Y, Trippodo N, Barrish J, Macor JE. Kowala MC, et al. Among authors: yang y. J Pharmacol Exp Ther. 2004 Apr;309(1):275-84. doi: 10.1124/jpet.103.055855. Epub 2004 Jan 12. J Pharmacol Exp Ther. 2004. PMID: 14718594
A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice.
Kang L, McIntyre KW, Gillooly KM, Yang Y, Haycock J, Roberts S, Khanna A, Herpin TF, Yu G, Wu X, Morton GC, Tuerdi H, Koplowitz B, Walker SG, Wardwell-Swanson J, Macor JE, Lawrence RM, Carlson KE. Kang L, et al. Among authors: yang y. J Leukoc Biol. 2006 Oct;80(4):897-904. doi: 10.1189/jlb.1204748. Epub 2006 Aug 3. J Leukoc Biol. 2006. PMID: 16888084
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