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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: vallgarda j. J Med Chem. 2010 Jun 10;53(11):4481-7. doi: 10.1021/jm100242d. J Med Chem. 2010. PMID: 20465278
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
Barf T, Vallgårda J, Emond R, Häggström C, Kurz G, Nygren A, Larwood V, Mosialou E, Axelsson K, Olsson R, Engblom L, Edling N, Rönquist-Nii Y, Ohman B, Alberts P, Abrahmsén L. Barf T, et al. Among authors: vallgarda j. J Med Chem. 2002 Aug 29;45(18):3813-5. doi: 10.1021/jm025530f. J Med Chem. 2002. PMID: 12190302