Discovery of novel sulfonamides as potent and selective inhibitors against human and mouse 11β-hydroxysteroid dehydrogenase type 1

@article{Xia2012DiscoveryON,
  title={Discovery of novel sulfonamides as potent and selective inhibitors against human and mouse 11$\beta$-hydroxysteroid dehydrogenase type 1},
  author={Guangxin Xia and L. Liu and Mengzhu Xue and Haiyan Liu and Jianxin Yu and Ping Li and Qian Chen and B. Xiong and Xuejun Liu and Jingkang Shen},
  journal={Molecular and Cellular Endocrinology},
  year={2012},
  volume={358},
  pages={46-52}
}
Several classes of non-steroid 11β-HSD1 inhibitors have been developed as promising treatments for Type 2 Diabetes (T2D). Using a human 11β-HSD1 selective inhibitor as a starting point, we designed and synthesized a new class of derivatives of 1-arylsulfonyl piperidine-3-carboxamides. It was found that the large lipophilic group on the amino moiety may lead to cross-species potency towards human and mouse, allowing drug development by evaluating compounds in rodent model. By exploring structure… Expand
Design, synthesis and SAR of piperidyl-oxadiazoles as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
Identification of novel 11β-HSD1 inhibitors by combined ligand- and structure-based virtual screening
Virtual screening applications in short-chain dehydrogenase/reductase research
...
1
2
...

References

SHOWING 1-10 OF 25 REFERENCES
Discovery of novel inhibitors of human 11β-hydroxysteroid dehydrogenase type 1
Potent and novel 11β-HSD1 inhibitors identified from shape and docking based virtual screening.
Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model.
11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development.
...
1
2
3
...