☆ 4.7 Article

Water-soluble pleuromutilin derivative with excellent in vitro and in vivo antibacterial activity against Gram-positive pathogens

JOURNAL OF MEDICINAL CHEMISTRY (2008)

期刊

JOURNAL OF MEDICINAL CHEMISTRY

卷 51, 期 7, 页码 1991-1994

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AMER CHEMICAL SOC

DOI: 10.1021/jm8000136

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Chemistry, Medicinal

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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 (similar to 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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