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Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.
Gu X, Dragovic J, Koo GC, Koprak SL, LeGrand C, Mundt SS, Shah K, Springer MS, Tan EY, Thieringer R, Hermanowski-Vosatka A, Zokian HJ, Balkovec JM, Waddell ST. Gu X, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5266-9. doi: 10.1016/j.bmcl.2005.08.052. Epub 2005 Sep 26. Bioorg Med Chem Lett. 2005. PMID: 16185866
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Aster SD, Graham DW, Kharbanda D, Patel G, Ponpipom M, Santorelli GM, Szymonifka MJ, Mundt SS, Shah K, Springer MS, Thieringer R, Hermanowski-Vosatka A, Wright SD, Xiao J, Zokian H, Balkovec JM. Aster SD, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2008 May 1;18(9):2799-804. doi: 10.1016/j.bmcl.2008.04.010. Epub 2008 Apr 9. Bioorg Med Chem Lett. 2008. PMID: 18434143
11beta-HSD1 inhibition ameliorates metabolic syndrome and prevents progression of atherosclerosis in mice.
Hermanowski-Vosatka A, Balkovec JM, Cheng K, Chen HY, Hernandez M, Koo GC, Le Grand CB, Li Z, Metzger JM, Mundt SS, Noonan H, Nunes CN, Olson SH, Pikounis B, Ren N, Robertson N, Schaeffer JM, Shah K, Springer MS, Strack AM, Strowski M, Wu K, Wu T, Xiao J, Zhang BB, Wright SD, Thieringer R. Hermanowski-Vosatka A, et al. Among authors: springer ms. J Exp Med. 2005 Aug 15;202(4):517-27. doi: 10.1084/jem.20050119. J Exp Med. 2005. PMID: 16103409 Free PMC article.
Benzamide derivatives as blockers of Kv1.3 ion channel.
Miao S, Bao J, Garcia ML, Goulet JL, Hong XJ, Kaczorowski GJ, Kayser F, Koo GC, Kotliar A, Schmalhofer WA, Shah K, Sinclair PJ, Slaughter RS, Springer MS, Staruch MJ, Tsou NN, Wong F, Parsons WH, Rupprecht KM. Miao S, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1161-4. doi: 10.1016/s0960-894x(03)00014-3. Bioorg Med Chem Lett. 2003. PMID: 12643934
Potent Kv1.3 inhibitors from correolide-modification of the C18 position.
Bao J, Miao S, Kayser F, Kotliar AJ, Baker RK, Doss GA, Felix JP, Bugianesi RM, Slaughter RS, Kaczorowski GJ, Garcia ML, Ha SN, Castonguay L, Koo GC, Shah K, Springer MS, Staruch MJ, Parsons WH, Rupprecht KM. Bao J, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2005 Jan 17;15(2):447-51. doi: 10.1016/j.bmcl.2004.10.058. Bioorg Med Chem Lett. 2005. PMID: 15603971
11β-HSD1 inhibition reduces atherosclerosis in mice by altering proinflammatory gene expression in the vasculature.
Luo MJ, Thieringer R, Springer MS, Wright SD, Hermanowski-Vosatka A, Plump A, Balkovec JM, Cheng K, Ding GJ, Kawka DW, Koo GC, Grand CB, Luo Q, Maletic MM, Malkowitz L, Shah K, Singer I, Waddell ST, Wu KK, Yuan J, Zhu J, Stepaniants S, Yang X, Lum PY, Wang IM. Luo MJ, et al. Among authors: springer ms. Physiol Genomics. 2013 Jan 7;45(1):47-57. doi: 10.1152/physiolgenomics.00109.2012. Epub 2012 Nov 20. Physiol Genomics. 2013. PMID: 23170035
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: springer ms. Bioorg Med Chem Lett. 2002 Oct 21;12(20):3001-4. doi: 10.1016/s0960-894x(02)00606-6. Bioorg Med Chem Lett. 2002. PMID: 12270193
723 results