Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.

@article{Palmer2006Keto134oxadiazolesAC,
  title={Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.},
  author={James Trevor Palmer and Bernard L. Hirschbein and Harry Cheung and John McCarter and James W. Janc and Zhen-ming Yu and Gregg A Wesolowski},
  journal={Bioorganic & medicinal chemistry letters},
  year={2006},
  volume={16 11},
  pages={
          2909-14
        }
}
We have prepared a series of cathepsin K inhibitors bearing the keto-1,3,4-oxadiazole warhead capable of forming a hemithioketal complex with the target enzyme. By modifying binding moieties at the P1, P2, and prime side positions of the inhibitors, we have achieved selectivity over cathepsins B, L, and S, and have achieved sub-nanomolar potency against cathepsin K. This series thus represents a promising chemotype that could be used in diseases implicated by imbalances in cathepsin K activity… CONTINUE READING
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