Structure− Activity Relationships of Substituted 1-Pyridyl-2-phenyl-1, 2-ethanediones: Potent, Selective Carboxylesterase Inhibitors

…, DC Bouck, T Chen, P Hanumesh, J Price…

文献索引：Young, Brandon M.; Hyatt, Janice L.; Bouck, David C.; Chen, Taosheng; Hanumesh, Parimala; Price, Jeanine; Boyd, Vincent A.; Potter, Philip M.; Webb, Thomas R. Journal of Medicinal Chemistry, 2010 , vol. 53, # 24 p. 8709 - 8715

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被引用次数: 8

摘要

Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/ pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1, 2-dione inhibitors are decidedly hydrophobic, a modified dione scaffold was designed and elaborated into a> 300 member library, which was subsequently screened to establish the SAR for esterase inhibition. This allowed the identification of ...