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Issue 30, 2012
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Synthesis of selective inhibitors against V. cholerae sialidase and human cytosolic sialidase NEU2

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Abstract

Sialidases or neuraminidases catalyze the hydrolysis of terminal sialic acid residues from sialyl oligosaccharides and glycoconjugates. Despite successes in developing potent inhibitors specifically against influenza virus neuraminidases, the progress in designing and synthesizing selective inhibitors against bacterial and human sialidases has been slow. Guided by sialidase substrate specificity studies and sialidase crystal structural analysis, a number of 2-deoxy-2,3-dehydro-N-acetylneuraminic acid (DANA or Neu5Ac2en) analogues with modifications at C9 or at both C5 and C9 were synthesized. Inhibition studies of various bacterial sialidases and human cytosolic sialidase NEU2 revealed that Neu5Gc9N32en and Neu5AcN39N32en are selective inhibitors against V. cholerae sialidase and human NEU2, respectively.

Graphical abstract: Synthesis of selective inhibitors against V. cholerae sialidase and human cytosolic sialidase NEU2

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Publication details

The article was received on 16 Feb 2012, accepted on 08 May 2012 and first published on 08 May 2012


Article type: Paper
DOI: 10.1039/C2OB25335F
Citation: Org. Biomol. Chem., 2012,10, 6112-6120
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    Synthesis of selective inhibitors against V. cholerae sialidase and human cytosolic sialidase NEU2

    Z. Khedri, Y. Li, H. Cao, J. Qu, H. Yu, M. M. Muthana and X. Chen, Org. Biomol. Chem., 2012, 10, 6112
    DOI: 10.1039/C2OB25335F

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