Tetrahedron

Synthesis, hydrolysis, biochemical and theoretical evaluation of 1, 4-bis (alkoxycarbonyl) azetidin-2-ones as potential elastase inhibitors

…, G Dive, B Clamot, R Touillaux, J Marchand-Brynaert

文献索引：Gerard, Stephane; Dive, Georges; Clamot, Brigitte; Touillaux, Roland; Marchand-Brynaert, Jacqueline Tetrahedron, 2002 , vol. 58, # 12 p. 2423 - 2433

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被引用次数: 42

摘要

A series of 1, 4-bis (alkoxycarbonyl) azetidin-2-ones, designed as potential suicide-inhibitors of serine proteases, has been synthesized and evaluated against porcine pancreatic elastase (PPE). The most active compound (Ki∼ 10μM; reversible inhibitor) was equipped with phenethyloxycarbonyl and benzyloxycarbonyl side-chains at positions N1 and C4, respectively, with the (S)-configuration. 1H NMR spectroscopic analysis of the reaction ...