Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV

  • Bioorg Med Chem Lett. 2013 May 15;23(10):2955-61. doi: 10.1016/j.bmcl.2013.03.047.
Mark J Mitton-Fry  1 ,  Steven J Brickner ,  Judith C Hamel ,  Lori Brennan ,  Jeffrey M Casavant ,  Michael Chen ,  Tao Chen ,  Xiaoyuan Ding ,  James Driscoll ,  Joel Hardink ,  Thuy Hoang ,  Erbing Hua ,  Michael D Huband ,  Meghan Maloney ,  Anthony Marfat ,  Sandra P McCurdy ,  Dale McLeod ,  Michael Plotkin ,  Usa Reilly ,  Shaughn Robinson ,  John Schafer ,  Richard M Shepard ,  James F Smith ,  Gregory G Stone ,  Chakrapani Subramanyam ,  Kwansik Yoon ,  Wei Yuan ,  Richard P Zaniewski ,  Christopher Zook
Affiliations
  • 1. Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA. [email protected]
PMID: 23566517 DOI: 10.1016/j.bmcl.2013.03.047
Abstract

A structurally novel set of inhibitors of Bacterial type II topoisomerases with potent in vitro and in vivo Antibacterial activity was developed. Dual-targeting ability, hERG inhibition, and pharmacokinetic properties were also assessed.