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ANTIBIOTIC AND ANTI-PARASITIC AGENTS THAT MODULATE CLASS II FRUCTOSE 1,6-BISPHOSPHATE ALDOLASE
专利权人:
发明人:
申请号:
EP14794723.8
公开号:
EP2994142A1
申请日:
2014.05.08
申请国别(地区):
EP
年份:
2016
代理人:
摘要:
This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds dont bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
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