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  • Title: Water-soluble pleuromutilin derivative with excellent in vitro and in vivo antibacterial activity against gram-positive pathogens.
    Author: Hirokawa Y, Kinoshita H, Tanaka T, Nakata K, Kitadai N, Fujimoto K, Kashimoto S, Kojima T, Kato S.
    Journal: J Med Chem; 2008 Apr 10; 51(7):1991-4. PubMed ID: 18330977.
    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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