New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
Copyright policy )New Tetromycin Derivatives with Anti-Trypanosomal and Protease Inhibitory Activities
Four new tetromycin derivatives, tetromycins 1–4 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.
- University of Bonn Germany
- University of Bonn Germany
- Health Sciences Centre Canada
- McMaster University (McMaster Centre for Software Certification) Canada
- Institute of Organic Chemistry Hungary
Magnetic Resonance Spectroscopy, anti-trypanosomal, QH301-705.5, Cathepsin L, Streptomyces axinellae, Trypanosoma brucei brucei, Antiprotozoal Agents, ddc:547, Heterocyclic Compounds, 4 or More Rings, Article, Cathepsin B, Viral Proteins, Axinella, Animals, Protease Inhibitors, Biology (General), Coronavirus 3C Proteases, Leishmania major, ddc:610, Trypanocidal Agents, Streptomyces, protease inhibition, Cysteine Endopeptidases, Severe acute respiratory syndrome-related coronavirus, tetromycin, <em>Streptomyces axinellae</em>, Biologie, marine sponge
Magnetic Resonance Spectroscopy, anti-trypanosomal, QH301-705.5, Cathepsin L, Streptomyces axinellae, Trypanosoma brucei brucei, Antiprotozoal Agents, ddc:547, Heterocyclic Compounds, 4 or More Rings, Article, Cathepsin B, Viral Proteins, Axinella, Animals, Protease Inhibitors, Biology (General), Coronavirus 3C Proteases, Leishmania major, ddc:610, Trypanocidal Agents, Streptomyces, protease inhibition, Cysteine Endopeptidases, Severe acute respiratory syndrome-related coronavirus, tetromycin, <em>Streptomyces axinellae</em>, Biologie, marine sponge
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