DNA binding ligands with improved in vitro and in vivo potency against drug-resistant Staphylococcus aureus.

Abstract

Potent in vivo activity against methicillin-resistant Staphylococcus aureus (MRSA) has been difficult to achieve with previously reported DNA binding antibacterials. Herein, we describe an efficient access to a focused library of new analogues yielding compounds with improved activity in a mouse peritonitis model. The most potent molecules (14 and 19) exhibit efficacy against MRSA at ED50 values of approximately 1 and approximately 5 mg/kg, respectively, and display excellent in vitro activity against vancomycin-resistant S. aureus.

Cite this paper

@article{Hu2004DNABL, title={DNA binding ligands with improved in vitro and in vivo potency against drug-resistant Staphylococcus aureus.}, author={Wenhao Hu and Roland W. B{\"{u}rli and Jacob A Kaizerman and Kirk Johnson and Matthew I Gross and Mari Iwamoto and Peter L. Jones and Denene Lofland and Stacey Difuntorum and Hsiu Man Chen and B{\"{u}lent Bozdoğan and Peter C. Appelbaum and Heinz E Moser}, journal={Journal of medicinal chemistry}, year={2004}, volume={47 18}, pages={4352-5} }