Towards calixarene-based prodrugs: Drug release and antibacterial behaviour of a water-soluble nalidixic acid/calix[4]arene ester adduct.
A water-soluble calixarene-based heterocyclic podand incorporating a quinolone antibiotic subunit, the nalidixic acid, was synthesised and fully characterised. Its prodrug behaviour was assessed in vitro by HPLC, demonstrating the release of the tethered quinolone in model biological conditions. Microbiological studies performed on various Gram-positive and Gram-negative reference strains showed very interesting antibacterial activities.
Dibama
Hugues Massimba
HM
SRSMC, UMR Nancy Université-CNRS, France.
Clarot
Igor
I
Fontanay
Stéphane
S
Salem
Adel Ben
AB
Mourer
Maxime
M
Finance
Chantal
C
Duval
Raphaël E
RE
Regnouf-de-Vains
Jean-Bernard
JB
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047250:Calixarenes / 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; D009268:Nalidixic Acid / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D010636:Phenols / Q000737:chemistry*; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D014867:Water / Q000737:chemistry
D000900:Anti-Bacterial Agents; D010636:Phenols; D011355:Prodrugs; C121325:calix(4)arene; D014867:Water; D047250:Calixarenes; D009268:Nalidixic Acid