Synthesis and Biological Evaluation of Novel 2-Substituted Analogues of (-)-Pentenomycin IZisopoulou, 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.
Research output: Contribution to journal › Article › Academic › peer-review
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.
|Number of pages||7|
|Publication status||Published - 17-Mar-2020|
- (-)-pentenomycin, Sonogashira, Suzuki, antimicrobial agents, Gram-positive bacteria, PENTENOMYCIN-I, DERIVATIVES