@article{APS6430,
author = {Xu Zhang and Yang Zhou and Yu Shen and Li-li Du and Jun-hua Chen and Ying Leng and Jian-hua Shen},
title = {Derivatives of (phenylsulfonamido-methyl)nicotine and (phenylsulfonamido-methyl)thiazole as novel 11β-hydroxysteroid dehydrogenase type 1 inhibitors: synthesis and biological activities in vitro},
journal = {Acta Pharmacologica Sinica},
volume = {30},
number = {9},
year = {2016},
keywords = {},
abstract = {Aim: To design and synthese a novel class of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors, featuring the (phenylsulfonamido-methyl)pyridine and (phenylsulfonamido-methyl)thiazole framework.
Methods: Our initial lead 4-(phenylsulfonamido-methyl)benzamides were modified. Inhibition of human and mouse 11β-HSD1 enzymatic activities by the new compounds was determined by a scintillation proximity assay (SPA) using microsomes containing 11β-HSD1.
Results: Sixteen new compounds (6a–6h, 7a–7h) were designed, synthesized and bioassayed. In dose-response studies, several compounds showed strong inhibitory activities with IC50 values at nanomolar or low nanomolar concentrations. Structure-activity relationships are also discussed with respect to molecular docking results.
Conclusion: This study provides two promising new templates for 11β-HSD1 inhibitors.},
issn = {1745-7254}, url = {http://www.chinaphar.com/article/view/6430}
}