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10.1021/ml300144n

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C4025654!4025654!24900382
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suck abstract from ncbi


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pmid24900382      ACS+Med+Chem+Lett 2012 ; 3 (10): 793-8
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  • Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11?-Hydroxysteroid Dehydrogenase Type 1 Inhibitors #MMPMID24900382
  • Yu J; Liu H; Xia G; Liu L; Xu Z; Chen Q; Ma C; Sun X; Xu J; Li H; Li P; Shi Y; Xiong B; Liu X; Shen J
  • ACS Med Chem Lett 2012[Oct]; 3 (10): 793-8 PMID24900382show ga
  • On the basis of scaffold hopping, a novel series of 2-alkyl-1-arylsulfonylprolinamides was discovered as 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD-1) inhibitors. A representative compound 4ek, obtained through SAR and structure optimization studies, demonstrates excellent in vitro potency against 11?-HSD-1 and dose-dependent in vivo inhibition of 11?-HSD-1 in a prednisone/prednisolone transformation biomarker study in mice.
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