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Page 1
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.
Maletic M, Leeman A, Szymonifka M, Mundt SS, Zokian HJ, Shah K, Dragovic J, Lyons K, Thieringer R, Vosatka AH, Balkovec J, Waddell ST. Maletic M, et al. Among authors: balkovec j. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2568-72. doi: 10.1016/j.bmcl.2011.01.018. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21421311
Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Olson S, Aster SD, Brown K, Carbin L, Graham DW, Hermanowski-Vosatka A, LeGrand CB, Mundt SS, Robbins MA, Schaeffer JM, Slossberg LH, Szymonifka MJ, Thieringer R, Wright SD, Balkovec JM. Olson S, et al. Among authors: balkovec jm. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4359-62. doi: 10.1016/j.bmcl.2005.06.040. Bioorg Med Chem Lett. 2005. PMID: 16039856
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: balkovec jm. 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: balkovec jm. 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: balkovec jm. J Exp Med. 2005 Aug 15;202(4):517-27. doi: 10.1084/jem.20050119. J Exp Med. 2005. PMID: 16103409 Free PMC article.
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: balkovec jm. Physiol Genomics. 2013 Jan 7;45(1):47-57. doi: 10.1152/physiolgenomics.00109.2012. Epub 2012 Nov 20. Physiol Genomics. 2013. PMID: 23170035
Rapid development of two factor IXa inhibitors from hit to lead.
Parker DL Jr, Walsh S, Li B, Kim E, Sharipour A, Smith C, Chen YH, Berger R, Harper B, Zhang T, Park M, Shu M, Wu J, Xu J, Dewnani S, Sherer EC, Hruza A, Reichert P, Geissler W, Sonatore L, Ellsworth K, Balkovec J, Greenlee W, Wood HB. Parker DL Jr, et al. Among authors: balkovec j. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2321-5. doi: 10.1016/j.bmcl.2015.04.025. Epub 2015 Apr 13. Bioorg Med Chem Lett. 2015. PMID: 25937013
51 results