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2-amino-1,3-thiazol-4(5H)-ones as potent and selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: enzyme-ligand co-crystal structure and demonstration of pharmacodynamic effects in C57Bl/6 mice.
Johansson L, Fotsch C, Bartberger MD, Castro VM, Chen M, Emery M, Gustafsson S, Hale C, Hickman D, Homan E, Jordan SR, Komorowski R, Li A, McRae K, Moniz G, Matsumoto G, Orihuela C, Palm G, Veniant M, Wang M, Williams M, Zhang J. Johansson L, et al. Among authors: chen m. J Med Chem. 2008 May 22;51(10):2933-43. doi: 10.1021/jm701551j. Epub 2008 Apr 18. J Med Chem. 2008. PMID: 18419108
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
Véniant MM, Hale C, Hungate RW, Gahm K, Emery MG, Jona J, Joseph S, Adams J, Hague A, Moniz G, Zhang J, Bartberger MD, Li V, Syed R, Jordan S, Komorowski R, Chen MM, Cupples R, Kim KW, St Jean DJ Jr, Johansson L, Henriksson MA, Williams M, Vallgårda J, Fotsch C, Wang M. Véniant MM, et al. Among authors: chen mm. J Med Chem. 2010 Jun 10;53(11):4481-7. doi: 10.1021/jm100242d. J Med Chem. 2010. PMID: 20465278
The discovery of 2-anilinothiazolones as 11beta-HSD1 inhibitors.
Yuan C, St Jean DJ Jr, Liu Q, Cai L, Li A, Han N, Moniz G, Askew B, Hungate RW, Johansson L, Tedenborg L, Pyring D, Williams M, Hale C, Chen M, Cupples R, Zhang J, Jordan S, Bartberger MD, Sun Y, Emery M, Wang M, Fotsch C. Yuan C, et al. Among authors: chen m. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6056-61. doi: 10.1016/j.bmcl.2007.09.070. Epub 2007 Sep 25. Bioorg Med Chem Lett. 2007. PMID: 17919905
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: chen m. J Med Chem. 2008 Dec 25;51(24):7953-67. doi: 10.1021/jm801073z. J Med Chem. 2008. PMID: 19053753
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