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Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
Aki C, Chao J, Ferreira JA, Dwyer MP, Yu Y, Chao J, Merritt RJ, Lai G, Wu M, Hipkin RW, Fan X, Gonsiorek W, Fosseta J, Rindgen D, Fine J, Lundell D, Taveras AG, Biju P. Aki C, et al. Among authors: gonsiorek w. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4446-9. doi: 10.1016/j.bmcl.2009.05.049. Epub 2009 May 18. Bioorg Med Chem Lett. 2009. PMID: 19525110
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies.
Shankar BB, Lavey BJ, Zhou G, Spitler JA, Tong L, Rizvi R, Yang DY, Wolin R, Kozlowski JA, Shih NY, Wu J, Hipkin RW, Gonsiorek W, Lunn CA. Shankar BB, et al. Among authors: gonsiorek w. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4417-20. doi: 10.1016/j.bmcl.2005.07.023. Bioorg Med Chem Lett. 2005. PMID: 16115769
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
Dwyer MP, Yu Y, Chao J, Aki C, Chao J, Biju P, Girijavallabhan V, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, Rokosz LL, Kaiser B, Li G, Wang W, Stauffer T, Ozgur L, Baldwin J, Taveras AG. Dwyer MP, et al. Among authors: gonsiorek w. J Med Chem. 2006 Dec 28;49(26):7603-6. doi: 10.1021/jm0609622. J Med Chem. 2006. PMID: 17181143
Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.
Yu Y, Dwyer MP, Chao J, Aki C, Chao J, Purakkattle B, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Qiu H, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, He Z, Lai G, Wu M, Taveras A. Yu Y, et al. Among authors: gonsiorek w. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1318-22. doi: 10.1016/j.bmcl.2008.01.024. Epub 2008 Jan 11. Bioorg Med Chem Lett. 2008. PMID: 18242983
Expansion of SAR studies on triaryl bis sulfone cannabinoid CB2 receptor ligands.
Tong L, Shankar BB, Chen L, Rizvi R, Kelly J, Gilbert E, Huang C, Yang DY, Kozlowski JA, Shih NY, Gonsiorek W, Hipkin RW, Malikzay A, Lunn CA, Lundell DJ. Tong L, et al. Among authors: gonsiorek w. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6785-9. doi: 10.1016/j.bmcl.2010.08.126. Epub 2010 Aug 31. Bioorg Med Chem Lett. 2010. PMID: 20850969
Murine CXCR1 is a functional receptor for GCP-2/CXCL6 and interleukin-8/CXCL8.
Fan X, Patera AC, Pong-Kennedy A, Deno G, Gonsiorek W, Manfra DJ, Vassileva G, Zeng M, Jackson C, Sullivan L, Sharif-Rodriguez W, Opdenakker G, Van Damme J, Hedrick JA, Lundell D, Lira SA, Hipkin RW. Fan X, et al. Among authors: gonsiorek w. J Biol Chem. 2007 Apr 20;282(16):11658-66. doi: 10.1074/jbc.M607705200. Epub 2006 Dec 29. J Biol Chem. 2007. PMID: 17197447 Free article.
A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation.
Chapman RW, Minnicozzi M, Celly CS, Phillips JE, Kung TT, Hipkin RW, Fan X, Rindgen D, Deno G, Bond R, Gonsiorek W, Billah MM, Fine JS, Hey JA. Chapman RW, et al. Among authors: gonsiorek w. J Pharmacol Exp Ther. 2007 Aug;322(2):486-93. doi: 10.1124/jpet.106.119040. Epub 2007 May 11. J Pharmacol Exp Ther. 2007. PMID: 17496165
28 results