Second generation analogs of rigid 6,7-spiro scaffolds targeting the bacterial ribosome

Previous work from our group described the synthesis and biological evaluation of new rigid, 6,6- and 6,7-spiro aminoglycosidic scaffolds targeting the bacterial ribosome. Herein we describe an improved synthetic protocol for their construction, and extend our study by further amino-functionalizatio...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (24), p.7488-7492
Hauptverfasser:	Stathakis, Christos I., Mavridis, Ioannis, Kythreoti, Georgia, Papakyriakou, Athanasios, Katsoulis, Ioannis A., Cottin, Thomas, Anastasopoulou, Panoula, Vourloumis, Dionisios
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminoglycosides Aminoglycosides - chemistry Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibiotics Antibiotics. Antiinfectious agents. Antiparasitic agents Bacteria Bacteria - genetics Binding Sites Biological and medical sciences Computer Simulation General aspects Medical sciences Pharmacology. Drug treatments Ribosomal RNA Ribosomes RNA, Ribosomal, 16S - chemistry RNA, Ribosomal, 16S - metabolism scaffolds Spiro Compounds - chemical synthesis Spiro Compounds - chemistry Spiro Compounds - pharmacology Spiro-compounds
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Zusammenfassung:	Previous work from our group described the synthesis and biological evaluation of new rigid, 6,6- and 6,7-spiro aminoglycosidic scaffolds targeting the bacterial ribosome. Herein we describe an improved synthetic protocol for their construction, and extend our study by further amino-functionalization of their 6,7-spiro analogs. The synthetic strategy, preparation and evaluation of some representative examples are reported.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.10.001