Journal
EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 23, Issue 9, Pages 1233-1237Publisher
INFORMA HEALTHCARE
DOI: 10.1517/13543776.2013.820707
Keywords
antibacterial; DNA gyrase; prodrugs; topoisomerase IV
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The two patent applications describe two novel compounds in the benzimidazole class of GyrB/ParE antibacterial agents and multiple phosphate prodrugs derived from these compounds. The new benzimidazole compounds have excellent antibacterial activity on Gram-positive strains. But like previous benzimidazoles, they have limited solubility and are highly protein bound. The phosphate prodrugs offer a drug substance with high aqueous solubility that should aid both intravenous and oral formulations. The potential utility of the prodrugs was demonstrated in efficacy studies.
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