Acyl Amino Acid Derivatives as Novel Inhibitors of Influenza Neuraminidase
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概要
- 論文の詳細を見る
We searched our chemical collection to identify non-N-acetylneuraminate (NeuAC) inhibitors of influenza neuraminidase (NA). Of the 62 acyl derivatives tested, several acyl amino acids, but not acyl alkanolamine derivatives, were effective and inhibited the NA activity in a dose-dependent manner. N-3-Hydroxymyristoyl D-cysteine and N-myristoyl-O-caproyl-D-serine were the more potent compounds and inhibited the enzyme in a noncompetitive manner (K_i=102 and 125 μM, respectively) without respect to the substrate. An important consideration for the choice of inhibitor is the selectivity of the inhibition. These compounds were selective inhibitors of viral NA and effective for any variant enzyme, but the enzymes from V. cholerae and human placenta were insensitive. Accordingly, the acyl amino acid derivatives may be expected to be inhibitors without cellular toxicity and may serve as lead compounds for anti-influenza agents.
- 社団法人日本農芸化学会の論文
- 1997-05-23
著者
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KATO Jyoji
Department of Surgery II, Nagoya City University Medical School
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Azuma Masayuki
Department of Agricultural Chemistry, Faculty of Agriculture, The University of Tokyo
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Ooshima Hiroshi
Dep. Of Applied Chemistry And Bioengineering Graduate School Of Engineering Osaka City Univ.
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Ooshima H
Osaka City Univ. Osaka Jpn
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Ooshima Hiroshi
Department Of Applied Chemistry And Bioengineering Graduate School Of Engineering Osaka City Univers
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Ooshima Hiroshi
Department Of Applied And Bioapplied Chemistry Graduate School Of Engineering Osaka City University
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Kato J
Department Of Applied Chemistry And Bioengineering Graduate School Of Engineering Osaka City Univers
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Kato Jyoji
Department Of Bioapplied Chemistry
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Azuma M
Department Of Applied Chemistry And Bioengineering Graduate School Of Engineering Osaka City Univers
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Azuma Masayuki
Second Department Of Oral And Maxillofacial Surgery Tokushima University School Of Dentistry
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KONDOH MITSUYO
Department of Bioapplied Chemistry, Osaka City University
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FURUTANI Toshiyuki
Pharmaceutical Development Research Laboratory, Tanabe Seiyaku Co., Ltd.
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Furutani T
Tanabe Seiyaku Co. Ltd. Osaka Jpn
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Furutani Toshiyuki
Pharmaceutical Developemnt Research Laboratory:tanabe Seiyaku Co. Ltd.
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Kondoh Mitsuyo
Department Of Bioapplied Chemistry Osaka City University
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Kato Jyoji
Department of Applied Chemistry and Bioengineering, Graduate School of Engineering, Osaka City University
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