Ontology highlight
ABSTRACT:
SUBMITTER: Gerasyuto AI
PROVIDER: S-EPMC5991783 | biostudies-literature | 2018 May
REPOSITORIES: biostudies-literature
Gerasyuto Aleksey I AI Arnold Michael A MA Wang Jiashi J Chen Guangming G Zhang Xiaoyan X Smith Sean S Woll Matthew G MG Baird John J Zhang Nanjing N Almstead Neil G NG Narasimhan Jana J Peddi Srinivasa S Dumble Melissa M Sheedy Josephine J Weetall Marla M Branstrom Arthur A AA Prasad J V N JVN Karp Gary M GM
Journal of medicinal chemistry 20180514 10
There exists an urgent medical need to identify new chemical entities (NCEs) targeting multidrug resistant (MDR) bacterial infections, particularly those caused by Gram-negative pathogens. 4-Hydroxy-2-pyridones represent a novel class of nonfluoroquinolone inhibitors of bacterial type II topoisomerases active against MDR Gram-negative bacteria. Herein, we report on the discovery and structure-activity relationships of a series of fused indolyl-containing 4-hydroxy-2-pyridones with improved in vi ...[more]