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Mar. Drugs 2011, 9(10), 1682-1697;

New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities

Julius-von-Sachs Institute for Biological Sciences, University of Würzburg, Julius-von-Sachs-Platz 3, Würzburg 97082, Germany
Institute for Pharmacy and Food Chemistry, Am Hubland, Würzburg 97074, Germany
Institute of Organic Chemistry, University of Würzburg, Am Hubland, Würzburg 97074, Germany
Department of Medicinal Chemistry, University of Utah, Salt Lake City, UT 84112, USA
This work is dedicated to Johannes F. Imhoff on the occasion of his 60th birthday.
Current address: Department of Biochemistry and Biomedical Sciences, Health Sciences Centre, McMaster University, 1200 Main St. W. Hamilton, ON L8N 3Z5, Canada.
Current address: Kekulé Institute of Organic Chemistry and Biochemistry, University of Bonn, Gerhard-Domagk-Str. 1, Bonn 53121, Germany.
Current address: School of Pharmacy, University of Wisconsin-Madison, Madison, WI 53705, USA.
Current address: Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, Mainz 55099, Germany.
Author to whom correspondence should be addressed.
Received: 25 July 2011 / Revised: 9 September 2011 / Accepted: 16 September 2011 / Published: 26 September 2011
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Four new tetromycin derivatives, tetromycins 14 and a previously known one, tetromycin B (5) were isolated from Streptomyces axinellae Pol001T 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 Mpro, and PLpro. The compounds showed antiparasitic activities against T. brucei and time-dependent inhibition of cathepsin L-like proteases with Ki values in the low micromolar range. View Full-Text
Keywords: tetromycin; anti-trypanosomal; protease inhibition; Streptomyces axinellae; marine sponge tetromycin; anti-trypanosomal; protease inhibition; Streptomyces axinellae; marine sponge
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Pimentel-Elardo, S.M.; Buback, V.; Gulder, T.A.; Bugni, T.S.; Reppart, J.; Bringmann, G.; Ireland, C.M.; Schirmeister, T.; Hentschel, U. New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities. Mar. Drugs 2011, 9, 1682-1697.

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