Serveur d'exploration SRAS

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New tetromycin derivatives with anti-trypanosomal and protease inhibitory activities.

Identifieur interne : 001449 ( PubMed/Curation ); précédent : 001448; suivant : 001450

New tetromycin derivatives with anti-trypanosomal and protease inhibitory activities.

Auteurs : Sheila M. Pimentel-Elardo [Allemagne] ; Verena Buback ; Tobias A M. Gulder ; Tim S. Bugni ; Jason Reppart ; Gerhard Bringmann ; Chris M. Ireland ; Tanja Schirmeister ; Ute Hentschel

Source :

RBID : pubmed:22072992

Descripteurs français

English descriptors

Abstract

Four new tetromycin derivatives, tetromycins 1-4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001(T) cultivated from the Mediterranean sponge Axinella polypoides. Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei, and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV M(pro), and PL(pro). The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with K(i) values in the low micromolar range.

DOI: 10.3390/md9101682
PubMed: 22072992

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Links to Exploration step

pubmed:22072992

Le document en format XML

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<div type="abstract" xml:lang="en">Four new tetromycin derivatives, tetromycins 1-4 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001(T) cultivated from the Mediterranean sponge Axinella polypoides. Structures were assigned using extensive 1D and 2D NMR spectroscopy as well as HRESIMS analysis. The compounds were tested for antiparasitic activities against Leishmania major and Trypanosoma brucei, and for protease inhibition against several cysteine proteases such as falcipain, rhodesain, cathepsin L, cathepsin B, and viral proteases SARS-CoV M(pro), and PL(pro). The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with K(i) values in the low micromolar range.</div>
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