Document Report Card

ID: ALA1142399

Journal: J Med Chem

Title: Water-soluble pleuromutilin derivative with excellent in vitro and in vivo antibacterial activity against gram-positive pathogens.

Authors: Hirokawa Y, Kinoshita H, Tanaka T, Nakata K, Kitadai N, Fujimoto K, Kashimoto S, Kojima T, Kato S.

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.

CiteXplore: 18330977

DOI: 10.1021/jm8000136