Potential protease inhibitors based on a functionalized cyclic sulfamide scaffold

Journal of Combinatorial Chemistry
Jiaying ZhongW C Groutas

Abstract

Exploratory studies related to the design and synthesis of functionalized cyclic sulfamides (I) as potential inhibitors of proteolytic enzymes were carried out. The structural motif and three diversity sites embodied in the scaffold render it amenable to combinatorial parallel synthesis and the facile generation of lead discovery prospecting libraries. The scaffold was readily assembled starting with (DL) serine methyl ester, and a series of compounds was generated and screened against human leukocyte elastase. Modification of the P(1) recognition element, believed to be accommodated at the primary specificity site (S(1) subsite) of the enzyme, yielded compounds that inhibited the enzyme by an apparent hyperbolic partial mixed-type inhibition.

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Citations

Dec 18, 2013·Chemical Reviews·William Spillane, Jean-Baptiste Malaubier
Feb 1, 2013·Organic Letters·Richard G CornwallYian Shi
Jun 19, 2013·Chemical Biology & Drug Design·Cindy J ChoyClifford E Berkman
Jan 1, 2006·Expert Opinion on Therapeutic Patents·Jean-Yves WinumClaudiu T Supuran
Nov 3, 2004·Bioorganic & Medicinal Chemistry·Jiaying ZhongWilliam C Groutas
May 20, 2006·Medicinal Research Reviews·Jean-Yves WinumClaudiu T Supuran
Nov 15, 2005·Journal of Combinatorial Chemistry·Roland E Dolle

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