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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: sudom a. J Med Chem. 2008 Jul 10;51(13):3953-60. doi: 10.1021/jm800310g. Epub 2008 Jun 14. J Med Chem. 2008. PMID: 18553955
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: sudom a. 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
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: sudom a. 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
Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Connors RV, Wang Z, Harrison M, Zhang A, Wanska M, Hiscock S, Fox B, Dore M, Labelle M, Sudom A, Johnstone S, Liu J, Walker NP, Chai A, Siegler K, Li Y, Coward P. Connors RV, et al. Among authors: sudom a. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3550-4. doi: 10.1016/j.bmcl.2009.04.151. Epub 2009 May 9. Bioorg Med Chem Lett. 2009. PMID: 19464171
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: sudom a. 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
26 results