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Updated: May 2, 2026

A Reference Broth Microdilution Method for Dalbavancin In Vitro Susceptibility Testing of Bacteria that Grow Aerobically
Published on: September 9, 2015
Water-soluble pleuromutilin derivative with excellent in vitro and in vivo antibacterial activity against
Yoshimi Hirokawa1, Hironori Kinoshita, Tomoyuki Tanaka
1Chemistry Research Laboratories, Dainippon Sumitomo Pharma Co. Ltd., Enoki 33-94, Suita, Osaka, 564-0053, Japan.
Abstract:
Although earlier pleuromutilin analogues showed potent in vitro antibacterial activity against some Gram-positive pathogens, their in vivo efficacy was low because of insufficient pharmacokinetic properties. We designed novel thioether pleuromutilin derivatives having a purine ring as a polar and water solubilizing group and identified a promising pleuromutilin analogue 6 with good solubility in water ( approximately 50 mg/mL). Compound 6 exhibited excellent in vitro and in vivo antibacterial activity against some Gram-positive strains, including drug-resistant pathogens.
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