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  • Title: Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).
    Author: 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.
    Journal: Bioorg Med Chem Lett; 2009 Mar 01; 19(5):1522-7. PubMed ID: 19181519.
    Abstract:
    The synthesis and SAR of a series of arylsulfonylpiperazine inhibitors of 11beta-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a cynomolgus monkey ex vivo enzyme inhibition model.
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