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

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.

Distribution of the usp gene in uropathogenic Escherichia coli isolated from companion animals and correlation with serotypes and size-variations of the pathogenicity island.

Uncomplicated urinary tract infection (UTI) caused by uropathogenic Escherichia coli(UPEC) is a serious problem not only among humans but also in companion animals such as dogs and cats. The uropathogenic specific protein gene (usp ) is preferentially distributed in UPEC isolates from dogs and cats compared with the distribution of usp in E. coli strains from feces of healthy dogs and cats and this pattern of distribution resembles that observed in human UPEC strains.