Iron transport-mediated drug delivery: practical syntheses and in vitro antibacterial studies of tris-catecholate siderophore-aminopenicillin conjugates reveals selectively potent antipseudomonal activity.
J Am Chem Soc
; 134(24): 9898-901, 2012 Jun 20.
Article
em En
| MEDLINE
| ID: mdl-22656303
ABSTRACT
An artificial tris-catecolate siderophore with a tripodal backbone and its conjugates with ampicillin and amoxicillin were synthesized. Both conjugates exhibited significantly enhanced in vitro antibacterial activities against Gram-negative species compared to the parent drugs, especially against Pseudomonas aeruginosa . The conjugates appeared to be assimilated by an induced bacterial iron transport process as their activities were inversely related to iron concentration. The easily synthesized tris-catecolate siderophore has great potential for future development of various drug conjugates to target antibiotic-resistant Gram-negative bacteria.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sideróforos
/
Bactérias Gram-Negativas
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Amoxicilina
/
Ampicilina
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Ferro
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Antibacterianos
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article
País de afiliação:
Estados Unidos