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Analogs of zanamivir with modified C4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses by Wen-Hsien Wen; Shi-Yun Wang; Keng-Chang Tsai; Yih-Shyun E. Cheng; An-Suei Yang; Jim-Min Fang; Chi-Huey Wong is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Unlike the group-2 neuraminidase, the group-1 neuraminidase of influenza virus possesses a flexible loop (the 150-loop) and a cavity (the 150-cavity) adjacent to the active site, and renders a conformational change from the 'open' form to the 'closed' form on binding with substrate (sialo-glycoprotein) or inhibitor (e.g., zanamivir). Zanamivir derivative 8a having an extended (piperazinocarbonyl)propyl substituent at the internal N-position of the guanidino group is designed as a possible inhibitor on the basis of computer docking to the open form of N1 subtype neuraminidase. Indeed, compound 8a exhibits strong neuraminidase inhibition and good anti-influenza activity against H1N1 virus with IC(50)=2.15microM and EC(50)=0.77microM, respectively. This study may provide a clue to future design of better group-1 neuraminidase inhibitors.

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Author

Wen-Hsien Wen; Shi-Yun Wang; Keng-Chang Tsai; Yih-Shyun E. Cheng; An-Suei Yang; Jim-Min Fang; Chi-Huey Wong

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)