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Synthesis and Biological Evaluation of Novel 2-Substituted Analogues of (-)-Pentenomycin I

Zisopoulou, S. A., Bousis, S., Haupenthal, J., Herrmann, J., Mueller, R., Hirsch, A. K. H., Komiotis, D., Gallos, J. K. & Stathakis, C. I., 17-Mar-2020, In : Synlett. 31, 5, p. 475-481 7 p.

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  • Synthesis and Biological Evaluation of Novel 2-Substituted ­Analogues of (–)-Pentenomycin I

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DOI

A library of novel 2-substituted derivatives of the antibiotic natural product pentenomycin I is presented. The new collection of analogues is divided in two main classes, 2-alkynyl- and 2-aryl- derivatives, which are accessed by the appropriate type of palladium-catalyzed cross-coupling reaction of the 2-iodo-protected pentenomycin I with suitable nucleophiles. The new derivatives were tested for their activity against certain types of bacteria and one of them, compound 8h , was found to exhibit significant inhibitory activity against several Gram-positive bacteria but also displayed cytotoxic activity against eukaryotic cell lines.

Original languageEnglish
Pages (from-to)475-481
Number of pages7
JournalSynlett
Volume31
Issue number5
Publication statusPublished - 17-Mar-2020

    Keywords

  • (-)-pentenomycin, Sonogashira, Suzuki, antimicrobial agents, Gram-positive bacteria, PENTENOMYCIN-I, DERIVATIVES

ID: 133208876