Journal
MOLECULES
Volume 19, Issue 5, Pages 6822-6837Publisher
MDPI AG
DOI: 10.3390/molecules19056822
Keywords
IMB-070593; prodrugs; synthesis; water solubility; antibacterial activity
Funding
- National S&T Major Special Project on Major New Drug Innovations [2012ZX09301002-001-017/023, 2014ZX09507009-003]
- NSFC [81373267-003]
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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.
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