Rigid spiroethers targeting the decoding center of the bacterial ribosome.
Continuing our efforts towards understanding the principles governing ribosomal recognition and function, we have synthesized and evaluated a series of diversely functionalized 5,6-, 6,6- and 7,6-spiroethers. These compounds successfully mimic natural aminoglycosides regarding their binding to the decoding center of the bacterial ribosome. Their potential to inhibit prokaryotic protein production in vitro along with their antibacterial potencies have also been examined.
Chemical Biology Laboratories, National Center for Scientific Research 'Demokritos', Agia Paraskevi Attikis, GR-15310, Greece.
Ioannis
I
Mavridis
Chemical Biology Laboratories, National Center for Scientific Research 'Demokritos', Agia Paraskevi Attikis, GR-15310, Greece.
Georgia
G
Kythreoti
Chemical Biology Laboratories, National Center for Scientific Research 'Demokritos', Agia Paraskevi Attikis, GR-15310, Greece.
Konstantina
K
Koltsida
Chemical Biology Laboratories, National Center for Scientific Research 'Demokritos', Agia Paraskevi Attikis, GR-15310, Greece. Electronic address: vourloumis@chem.demokritos.gr.
Dionisios
D
Vourloumis
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D004988:Ethers, Cyclic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D056004:Molecular Dynamics Simulation; D017434:Protein Structure, Tertiary; D012336:RNA, Ribosomal, 16S / Q000737:chemistry / Q000378:metabolism; D012270:Ribosomes / Q000737:chemistry / Q000378:metabolism*; D013141:Spiro Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D004988:Ethers, Cyclic; D012336:RNA, Ribosomal, 16S; D013141:Spiro Compounds; C531272:spiroether
Aminoglycosides; Antibacterials; RNA recognition; Ribosomal A-site; Spiroethers