Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
KK Adkison, DG Barrett, DN Deaton, RT Gampe…
文献索引：Adkison, Kim K.; Barrett, David G.; Deaton, David N.; Gampe, Robert T.; Hassell, Anne M.; Long, Stacey T.; McFadyen, Robert B.; Miller, Aaron B.; Miller, Larry R.; Payne, J. Alan; Shewchuk, Lisa M.; Wells-Knecht, Kevin J.; Willard Jr., Derril H.; Wright, Lois L. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 4 p. 978 - 983
Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme ...
