2940-24-1Relevant academic research and scientific papers
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.
Di-heterocyclic compounds and their use as antiviral agents
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, (2008/06/13)
Compounds of the formulas: STR1 wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed.
