18735-74-5Relevant articles and documents
A mild high yielding synthesis of oxazole-4-carboxylate derivatives
Ferreira, Paula M.T.,Castanheira, Elisabete M.S.,Monteiro, Luís S.,Pereira, Goreti,Vilaa, Helena
experimental part, p. 8672 - 8680 (2011/01/04)
Several 2,5-disubstituted oxazole-4-carboxylates were prepared in high yields from the methyl esters of N-acyl-β-halodehydroaminobutyric acid derivatives by treatment with a 2% solution of DBU in acetonitrile. The scope of this reaction was investigated a
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.
Syntheses of amamistatin fragments and determination of their HDAC and antitumor activity
Fennell, Kelley A.,Miller, Marvin J.
, p. 1683 - 1685 (2008/02/02)
Amamistatins A and B are natural products found to have anti-proliferative effects against MCF-7, A549, and MKN45 human tumor cell lines (IC50 0.24-0.56 μM). It was proposed that their activity was due to histone deacetylase (HDAC) inhibition m