Discovery of Azaindole Ureas as a Novel Class of Bacterial Gyrase B Inhibitors

Jing Zhang, Qingyi Yang, Jason B. Cross, Jan Antoinette C. Romero, Katherine M. Poutsiaka, Felix Epie, Douglas Bevan, Bin Wang, Yanzhi Zhang, Ajit Chavan, Xin Zhang, Terence Moy, Anu Daniel, Kien Nguyen, Brian Chamberlain, Nicole Carter, Joseph Shotwell, Jared Silverman, Chester A. Metcalf, Dominic RyanBlaise Lippa, Roland E. Dolle

Research output: Contribution to journalArticlepeer-review

19 Scopus citations


The emergence and spread of multidrug resistant bacteria are widely believed to endanger human health. New drug targets and lead compounds exempt from cross-resistance with existing drugs are urgently needed. We report on the discovery of azaindole ureas as a novel class of bacterial gyrase B inhibitors and detail the story of their evolution from a de novo design hit based on structure-based drug design. These inhibitors show potent minimum inhibitory concentrations against fluoroquinolone resistant MRSA and other Gram-positive bacteria.

Original languageEnglish
Pages (from-to)8503-8512
Number of pages10
JournalJournal of Medicinal Chemistry
Issue number21
StatePublished - Oct 13 2015


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