Potent and selective nonpeptidic inhibitors of procollagen C-proteinase

…, MG Collis, D Greiling, K James, J Kendall…

文献索引：Fish, Paul V.; Allan, Gillian A.; Bailey, Simon; Blagg, Julian; Butt, Richard; Collis, Michael G.; Greiling, Doris; James, Kim; Kendall, Jackie; McElroy, Andrew; McCleverty, Dawn; Reed, Charlotte; Webster, Robert; Whitlock, Gavin A. Journal of Medicinal Chemistry, 2007 , vol. 50, # 15 p. 3442 - 3456

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被引用次数: 37

摘要

6-Cyclohexyl-N-hydroxy-3-(1, 2, 4-oxadiazol-5-yl) hexanamides were previously disclosed as inhibitors of procollagen C-proteinase (PCP) culminating in the identification of amide 1. Our objective was to discover a second inhibitor that would have improved affinity for PCP and to optimize properties for transepidermal delivery (TED) to intact skin. Further investigation of this template identified a number of potent PCP inhibitors (IC50 values of 2 ...