Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: Intelligent design and evolution …

PS Charifson, AL Grillot, TH Grossman…

Index: Charifson, Paul S.; Grillot, Anne-Laure; Grossman, Trudy H.; Parsons, Jonathan D.; Badia, Michael; Bellon, Steve; Deininger, David D.; Drumm, Joseph E.; Gross, Christian H.; LeTiran, Arnaud; Liao, Yusheng; Mani, Nagraj; Nicolau, David P.; Perola, Emanuele; Ronkin, Steven; Shannon, Dean; Swenson, Lora L.; Tang, Qing; Tessier, Pamela R.; Tian, Ski-Kai; Trudeau, Martin; Wang, Tiansheng; Wei, Yunyi; Zhang, Hong; Stamos, Dean Journal of Medicinal Chemistry, 2008 , vol. 51, # 17 p. 5243 - 5263

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Citation Number: 140

Abstract

The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA gyrase and topoisomerase IV are well-characterized clinically validated targets of the fluoroquinolone antibiotics which exert their antibacterial activity through inhibition of the catalytic subunits. Inhibition of these targets through interaction ...