Hydrophobic benzoic acids as inhibitors of influenza neuraminidase.

Atigadda VR; Brouillette WJ; Duarte FBabu YSBantia SChand PChu NMontgomery JAWalsh DASudbeck EFinley JAir GMLuo MLaver GW

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Hydrophobic benzoic acids as inhibitors of influenza neuraminidase.

机译：Hydrophobic benzoic acids as inhibitors of influenza neuraminidase.

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Neuraminidase (NA) plays a critical role in the life cycle of influenza virus and is a target for new therapeutic agents. A new benzoic acid inhibitor (11) containing a lipophilic side chain at C-3 and a guanidine at C-5 was synthesized. The X-ray structure of 4-(N-acetylamino)-5-guanidino-3-(3-pentyloxy)benzoic acid in complex with NA revealed that the lipophilic side chain binds in a newly created hydrophobic pocket formed by the movement of Glu 278 to interact with Arg 226, whereas the guanidine of 11 interacts in a negatively charged pocket created by Asp 152, Glu 120 and Glu 229. Compound 11 was highly selective for type A (H2N2) influenza NA (IC50 1 microM) over type B (B/Lee/40) influenza NA (IC50 500 microM).

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来源
《Bioorganic and medicinal chemistry》 |1999年第11期|2487-2497|共11页
作者
Atigadda VR; Brouillette WJ; Duarte FBabu YSBantia SChand PChu NMontgomery JAWalsh DASudbeck EFinley JAir GMLuo MLaver GW;
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作者单位

Department of Chemistry, University of Alabama at Birmingham, 35294, USA.;

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原文格式 PDF
正文语种英语
中图分类药学;生物化学;
关键词
Benzoic Acids; Neuraminidase; Orthomyxoviridae; Antiviral Agents; Enzyme Inhibitors; 苯甲酸类; 神经氨酸酶; 正粘病毒科;

Hydrophobic benzoic acids as inhibitors of influenza neuraminidase.

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