Synthesis and antibacterial activity of amino acid and dipeptide prodrugs of IMB-070593, a fluoroquinolone candidate.
Molecules
; 19(5): 6822-37, 2014 May 23.
Article
in En
| MEDLINE
| ID: mdl-24858269
ABSTRACT
A series of amino acid and dipeptide prodrugs of IMB-070593, a fluoroquinolone candidate discovered in our lab, were synthesized and evaluated for their water solubility and then antibacterial activity. Our results reveal that four amino acid prodrugs 4a,b,e,f and two dipeptide prodrugs 4k,l have much greater solubility (>85 mg/mL) than IMB-070593 mesylate (22.5 mg/mL). Compounds 4a and 4k show good in vivo efficacy against MSSA 12-1 (p.o./i.v., 5.32-7.68 mg/kg) and S. pneumoniae12-10 (p.o., 18.39-23.13 mg/kg) which is 1.19-1.50 fold more active than the parent drug.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Oximes
/
Piperidines
/
Prodrugs
/
Dipeptides
/
Anti-Bacterial Agents
Limits:
Animals
Language:
En
Journal:
Molecules
Journal subject:
BIOLOGIA
Year:
2014
Document type:
Article
Affiliation country:
China