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

Basic Information

ID: ALA3734679

Journal: J Med Chem

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

Authors: Zhang J, Yang Q, Cross JB, Romero JA, Poutsiaka KM, Epie F, Bevan D, Wang B, Zhang Y, Chavan A, Zhang X, Moy T, Daniel A, Nguyen K, Chamberlain B, Carter N, Shotwell J, Silverman J, Metcalf CA, Ryan D, Lippa B, Dolle RE.

Abstract: 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.

CiteXplore: 26460684

DOI: 10.1021/acs.jmedchem.5b00961

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