Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)

…, Z Wang, M Cardozo, R Choi, M DeGraffenreid…

Index: Sun, Daqing; Wang, Zhulun; Cardozo, Mario; Choi, Rebekah; DeGraffenreid, Michael; Di, Yongmei; He, Xiao; Jaen, Juan C.; Labelle, Marc; Liu, Jinsong; Ma, Ji; Miao, Shichang; Sudom, Athena; Tang, Liang; Tu, Hua; Ursu, Stefania; Walker, Nigel; Yan, Xuelei; Ye, Qiuping; Powers, Jay P. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 5 p. 1522 - 1527

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Citation Number: 14

Abstract

Download PDF Opens in a new window. Article suggestions will be shown in a dialog on return to ScienceDirect. ... Please enable JavaScript to use all the features on this page. ... The synthesis and SAR of a series of arylsulfonylpiperazine inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a cynomolgus monkey ex vivo enzyme inhibition model. ... The synthesis and SAR of a series of ...