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Page 1
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).
Sun D, Wang Z, Cardozo M, Choi R, Degraffenreid M, Di Y, He X, Jaen JC, Labelle M, Liu J, Ma J, Miao S, Sudom A, Tang L, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP. Sun D, et al. Among authors: ye q. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1522-7. doi: 10.1016/j.bmcl.2008.12.114. Epub 2009 Jan 9. Bioorg Med Chem Lett. 2009. PMID: 19181519
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.
Julian LD, Wang Z, Bostick T, Caille S, Choi R, DeGraffenreid M, Di Y, He X, Hungate RW, Jaen JC, Liu J, Monshouwer M, McMinn D, Rew Y, Sudom A, Sun D, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP. Julian LD, et al. Among authors: ye q. J Med Chem. 2008 Jul 10;51(13):3953-60. doi: 10.1021/jm800310g. Epub 2008 Jun 14. J Med Chem. 2008. PMID: 18553955
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
McMinn DL, Rew Y, Sudom A, Caille S, Degraffenreid M, He X, Hungate R, Jiang B, Jaen J, Julian LD, Kaizerman J, Novak P, Sun D, Tu H, Ursu S, Walker NP, Yan X, Ye Q, Wang Z, Powers JP. McMinn DL, et al. Among authors: ye q. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1446-50. doi: 10.1016/j.bmcl.2009.01.026. Epub 2009 Jan 15. Bioorg Med Chem Lett. 2009. PMID: 19185488
The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors.
Yan X, Wang Z, Sudom A, Cardozo M, DeGraffenreid M, Di Y, Fan P, He X, Jaen JC, Labelle M, Liu J, Ma J, McMinn D, Miao S, Sun D, Tang L, Tu H, Ursu S, Walker N, Ye Q, Powers JP. Yan X, et al. Among authors: ye q. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7071-5. doi: 10.1016/j.bmcl.2010.09.097. Epub 2010 Sep 29. Bioorg Med Chem Lett. 2010. PMID: 20971000
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.
Sun D, Wang Z, Caille S, DeGraffenreid M, Gonzalez-Lopez de Turiso F, Hungate R, Jaen JC, Jiang B, Julian LD, Kelly R, McMinn DL, Kaizerman J, Rew Y, Sudom A, Tu H, Ursu S, Walker N, Willcockson M, Yan X, Ye Q, Powers JP. Sun D, et al. Among authors: ye q. Bioorg Med Chem Lett. 2011 Jan 1;21(1):405-10. doi: 10.1016/j.bmcl.2010.10.129. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21093258
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Fotsch C, Bartberger MD, Bercot EA, Chen M, Cupples R, Emery M, Fretland J, Guram A, Hale C, Han N, Hickman D, Hungate RW, Hayashi M, Komorowski R, Liu Q, Matsumoto G, St Jean DJ Jr, Ursu S, Véniant M, Xu G, Ye Q, Yuan C, Zhang J, Zhang X, Tu H, Wang M. Fotsch C, et al. Among authors: ye q. J Med Chem. 2008 Dec 25;51(24):7953-67. doi: 10.1021/jm801073z. J Med Chem. 2008. PMID: 19053753
5,348 results