Synthesis of dehydrodipeptide esters and their evaluation as inhibitors of cathepsin CReportar como inadecuado




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Medicinal Chemistry Research

, Volume 24, Issue 8, pp 3157–3165

First Online: 16 April 2015Received: 07 October 2014Accepted: 27 February 2015

Abstract

The procedures for the synthesis of esters of dehydropeptides containing C-terminal Z-dehydrophenylalanine and dehydroalanine have been elaborated. These esters appeared to be moderate or weak inhibitors of cathepsin C, with some of them exhibiting slow-binding behavior. As shown by molecular modeling, they are rather bound at the surface of the enzyme and are not submersed in its binding cavities.

KeywordsDehydropeptides Esterification Enzyme inhibitors Molecular modeling Electronic supplementary materialThe online version of this article doi:10.1007-s00044-015-1366-0 contains supplementary material, which is available to authorized users.

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Autor: Maciej Makowski - Paweł Lenartowicz - Bartosz Oszywa - Michał Jewgiński - Małgorzata Pawełczak - Paweł Kafarski

Fuente: https://link.springer.com/







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