Synthesis of macrocyclic, potential protease inhibitors using a generic scaffold

…, RFW Jackson, AB McElroy, J Overington…

文献索引：Dumez, Estelle; Snaith, John S.; Jackson, Richard F. W.; McElroy, Andrew B.; Overington, John; Wythes, Martin J.; Withka, Jane M.; McLellan, Thomas J. Journal of Organic Chemistry, 2002 , vol. 67, # 14 p. 4882 - 4892

全文：HTML全文

被引用次数: 35

摘要

A generic macrocyclic peptide structure 2 was designed as a potential inhibitor of a range of proteinases, by using as a basis for the design the known structures of a series of enzyme- inhibitor complexes. The macrocyclic nature of the target 2 was chosen so as to reduce the entropic advantage in the hydrolytic enzymatic step, and thereby to inhibit the function of the enzyme. The nature of the linking group was identified as a benzoxazole by molecular ...