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A synthetic method for diversification of the P1′ substituent in phosphinic dipeptides as a tool for exploration of the specificity of the S1′ binding pockets of leucine …

S Vassiliou, M Xeilari, A Yiotakis, J Grembecka…

文献索引:Vassiliou, Stamatia; Xeilari, Metaxia; Yiotakis, Athanasios; Grembecka, Jolanta; Pawelczak, Malgorzata; Kafarski, Pawel; Mucha, Artur Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 9 p. 3187 - 3200

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被引用次数: 26

摘要

A novel, general, and versatile method of diversification of the P1′ position in phosphinic pseudodipeptides, presumable inhibitors of proteolytic enzymes, was elaborated. The procedure was based on parallel derivatization of the amino group in the suitably protected phosphinate building blocks with appropriate alkyl and aryl halides. This synthetic strategy represents an original approach to phosphinic dipeptide chemistry. Its usefulness was ...