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New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities

Please always quote using this URN: urn:nbn:de:bvb:20-opus-141171
  • 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 proteasesFour 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.show moreshow less

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Metadaten
Author: Sheila M. Pimentel-Elardo, Verena Buback, Tobias A. M. Gulder, Tim S. Bugni, Jason Reppart, Gerhard Bringmann, Chris M. Ireland, Tanja Schirmeister, Ute Hentschel
URN:urn:nbn:de:bvb:20-opus-141171
Document Type:Journal article
Faculties:Fakultät für Biologie / Julius-von-Sachs-Institut für Biowissenschaften
Fakultät für Chemie und Pharmazie / Institut für Organische Chemie
Fakultät für Chemie und Pharmazie / Institut für Pharmazie und Lebensmittelchemie
Language:English
Parent Title (English):Marine drugs
Year of Completion:2011
Volume:9
Issue:10
Pagenumber:1682-1697
Source:Mar. Drugs 2011, 9, 1682-1697; doi:10.3390/md9101682
DOI:https://doi.org/10.3390/md9101682
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 54 Chemie / 547 Organische Chemie
Tag:Streptomyces axinellae; anti-trypanosomal; cysteine protease; discovery; drugs; marine sponge; protease inhibition; streptomyces; tetromycin
Release Date:2019/01/07
Licence (German):License LogoCC BY: Creative-Commons-Lizenz: Namensnennung