Perhydroquinolylbenzamides as novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

@article{Coppola2005PerhydroquinolylbenzamidesAN,
  title={Perhydroquinolylbenzamides as novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.},
  author={G. Coppola and P. Kukkola and J. Stanton and A. Neubert and N. Marcopulos and N. Bilci and Hua Wang and H. Tomaselli and Jenny Tan and T. Aicher and D. C. Knorr and A. Jeng and B. Dardik and R. Chatelain},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 21},
  pages={
          6696-712
        }
}
High-throughput screening identified 5 as a weak inhibitor of 11beta-HSD1. Optimization of the structure led to a series of perhydroquinolylbenzamides, some with low nanomolar inhibitory potency. A tertiary benzamide is required for biological activity and substitution of the terminal benzamide with either electron-donating or -withdrawing groups is tolerated. The majority of the compounds show selectivity of >20 to >700-fold over 11beta-HSD2. Analogues which showed >50% inhibition of 11beta… Expand
35 Citations
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors.
Discovery of adamantane ethers as inhibitors of 11beta-HSD-1: Synthesis and biological evaluation.
...
1
2
3
4
...