1016644-79-3Relevant academic research and scientific papers
Chemical inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
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Page/Page column 8, (2010/02/17)
The invention relates to new compounds having heptose synthesis inhibitory properties, of formula (I) or a pharmaceutically acceptable salt, or prodrug thereof, wherein A is an aryl or heterocycle, optionally substituted by one or several identical or different R such as H, C1-C10 alkyl, C1-C10 alkyl-OR1, C1-C10 alkyl-NR1R1, alkoxy, hydroxy, thioalkyl, aryl, heterocycle, halogen, nitro, cyano, CO2R1, NR1R1, NR1C(O)R1, C(O)NR1R1, NR1C(S)R1, C(S)NR1R1, SO2NR1R1, SO2R1, NR1SO2R1, NR1C(O)NR1R1, NR1C(O)OR1, NR1C(S)NR1R1, NR1C(S)OR1, R1C═NOR1, C(O)R1, aryloxy, thioaryl, alkenyl, alkynyl R1 identical or different is H or C1-C10 alkyl B1, B2, B3 identical or not represent C, N, O, S to form a five-membered aromatic ring wherein from one to three carbon atoms are replaced by a heteroatom selected from S, O, N optionally substituted by one or several identical or different R such as defined above B4 is C or N Y is H, C1-C10 alkyl, alkoxy, thio-alkyl, optionally substituted by one or several identical or different R such as defined above W is C, O or N, substituted or not by one or several C1-C10 alkyl radicals D is an heterocycle optionally substituted by one or several identical or different R such as defined above.
Towards Gram-negative antivirulence drugs: New inhibitors of HldE kinase
Desroy, Nicolas,Moreau, Francois,Briet, Sophia,Fralliec, Geraldine Le,Floquet, Stephanie,Durant, Lionel,Vongsouthi, Vanida,Gerusz, Vincent,Denis, Alexis,Escaich, Sonia
experimental part, p. 1276 - 1289 (2009/07/11)
Gram-negative bacteria lacking heptoses in their lipopolysaccharide (LPS) display attenuated virulence and increased sensitivity to human serum and to some antibiotics. Thus inhibition of bacterial heptose synthesis represents an attractive target for the development of new antibacterial agents. HldE is a bifunctional enzyme involved in the synthesis of bacterial heptoses. Development of a biochemical assay suitable for high-throughput screening allowed the discovery of inhibitors 1 and 2 of HldE kinase. Study of the structure-activity relationship of this series of inhibitors led to highly potent compounds.
