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-functionalization of their 6,7-spiro analogs. The synthetic strategy, preparation and evaluation of some representative examples are reported.
Laboratory of Chemical Biology of Natural Products and Designed Molecules, Institute of Physical Chemistry, NCSR DEMOKRITOS, Athens, Greece.
Christos I
CI
Stathakis
Ioannis
I
Mavridis
Georgia
G
Kythreoti
Athanasios
A
Papakyriakou
Ioannis A
IA
Katsoulis
Thomas
T
Cottin
Panoula
P
Anastasopoulou
Dionisios
D
Vourloumis
D000617:Aminoglycosides / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001419:Bacteria / Q000235:genetics*; D001665:Binding Sites; D003198:Computer Simulation; D012336:RNA, Ribosomal, 16S / Q000737:chemistry* / Q000378:metabolism; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D012336:RNA, Ribosomal, 16S; D013141:Spiro Compounds