Article
Antibacterial FabH Inhibitors with Mode of Action Validated in Haemophilus influenzae by in Vitro Resistance Mutation Mapping.
ACS infectious diseases - 8 Jul 2016
McKinney David C, Eyermann Charles J, Gu Rong-Fang, Hu Jun, Kazmirski Steven L, Lahiri Sushmita D, McKenzie Andrew R, Shapiro Adam B, Breault Gloria
Abstract excerpt
Fatty acid biosynthesis is essential to bacterial growth in Gram-negative pathogens. Several small molecules identified through a combination of high-throughput and fragment screening were cocrystallized with FabH (β-ketoacyl-acyl carrier protein synthase III) from Escherichia coli and Streptococcus pneumoniae. Structure-based drug design was used to merge several scaffolds to provide a new class of inhibitors....
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