Beta-lactam antibiotics functionalized with gem-bisphosphonates.
Acylation of amoxycillin and cephalexin with acids III, V and VII, and with isocyanate VIII furnished the corresponding beta-lactam antibiotics (X and XIII-XV, respectively). The antibacterial activity of these new antibiotic analogues against Helicobacter pylori was found to be identical with those of amoxycillin, Augmentin, erythromycin and ciprofloxacin.
Hornyák
M
M
Research Group of Antibiotics, Hungarian Academy of Sciences, L. Kossuth University, Debrecen, Hungary.
Hartmann
J F
JF
Sztaricskai
F J
FJ
Koncz
A
A
Hernádi
F
F
D000215:Acylation; D000658:Amoxicillin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002506:Cephalexin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D016480:Helicobacter pylori / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D063065:Organophosphonates; D013211:Staphylococcus aureus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D063065:Organophosphonates; D000658:Amoxicillin; D002506:Cephalexin