Synthesis and evaluation of 4-O-alkylated 2-deoxy-2,3-didehydro-N-acetylneuraminic acid derivatives as inhibitors of human parainfluenza virus type-3 sialidase activity
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Dyason, Jeffrey C
Thomson, Robin J
Suzuki, Takashi
Ueyama, Hiroo
Kuwahara, Yohta
Maki, Naoyoshi
Suzuki, Yasuo
von Itzstein, Mark
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Boger, D. L.
Ghosez, L.
Shibasaki, M.
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Abstract
The X-ray crystal structure of the paramyxoviral surface glycoprotein haemagglutinin-neuraminidase (HN) from Newcastle Disease virus was used as a template to design inhibitors of the HN from human parainfluenza virus type-3 (hPIV-3). 4-O-Alkylated derivatives of 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (Neu5Ac2en), accessed from 8,9-O-isopropylidenated-Neu5Ac2en1Me, were found to inhibit the sialidase (neuraminidase) activity of hPIV-3 (strain C243) in the range of 3-30 卮 This is comparable or improved activity compared to the parent 4-hydroxy compound.
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Bioorganic & Medicinal Chemistry Letters
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17
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Medicinal and biomolecular chemistry
Organic chemistry
Pharmacology and pharmaceutical sciences