In 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 published 《Antibacterial FabH Inhibitors with Mode of Action Validated in Haemophilus influenzae by in Vitro Resistance Mutation Mapping》.ACS Infectious Diseases published the findings.Synthetic Route of C5H3BrClN The information in the text is summarized as follows:
Fatty acid biosynthesis is essential to bacterial growth in Gram-neg. pathogens. Several small mols. identified through a combination of high-throughput and fragment screening were cocrystd. 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. After optimization for Gram-neg. enzyme inhibitory potency, several compounds demonstrated antimicrobial activity against an efflux-neg. strain of Haemophilus influenzae. Mutants resistant to these compounds had mutations in the FabH gene near the catalytic triad, validating FabH as a target for antimicrobial drug discovery.5-Bromo-2-chloropyridine(cas: 53939-30-3Synthetic Route of C5H3BrClN) was used in this study.
5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Synthetic Route of C5H3BrClN