Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Syntheses of 2-Deoxy-2,3-didehydro-N-acetylneuraminic Acid Analogues Modified by α-Acylaminoamido Groups at the C-4 Position Using Isocyanide-Based Four-Component Coupling and Biological Evaluation as Inhibitors of Human Parainfluenza Virus Type 1
Reiko NishinoTakuya HayakawaTadanobu TakahashiTakashi SuzukiMasayuki SatoKiyoshi Ikeda
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2013 Volume 61 Issue 1 Pages 69-74

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Abstract

Novel sialidase inhibitors 11 having an α-acylaminoamido group at the C-4 position of Neu5Ac2en 1 against human parainfluenza virus type 1 (hPIV-1) were synthesized using one-pot isocyanide-based four-component condensation, and their inhibitory activities against hPIV-1 sialidase were studied. Compound 11b showed inhibitory activity (IC50=5.1 mM) against hPIV-1 sialidase. The degree of inhibition of 11b was much weaker than that of 1 (IC50=0.3 mM).

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© 2013 The Pharmaceutical Society of Japan
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