title: Evaluation of a Set of C9 N-acyl Neu5Ac2en Mimetics as Viral Sialidase Selective Inhibitors.
abstract: Identification of selective influenza viral sialidase inhibitors is highly desirable in order to minimize or avoid the adverse effects due to the possible inhibition of endogenous human sialidases. We recently reported the evaluation of C9 N-acyl Neu5Ac2en mimetics as probes for human sialidases. Herein, we describe the in vitro activity of the same set of C9 N-acyl Neu5Ac2en mimetics against sialidases expressed by influenza virus A/PR/8/34 (H1N1), A/Memphis/1/72 (H3N2), and A/Duck/313/78 (H5N3) strains. Compound 8 is identified as a promising starting point for the development of viral sialidase selective inhibitors. Multiple sequence alignment and molecular docking techniques are also performed to explore the plausible interaction of compound 8 with viral sialidases.
authors.affiliation: Department of Applied Bioorganic Chemistry, Faculty of Applied Biological Sciences, Gifu University, Gifu, Japan; Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, USA.
authors.forename: Sadagopan
authors.initials: S
authors.lastname: Magesh
authors.affiliation: Faculty of Medicine, Thammasat University (Rangsit Campus), Pathumthani, Thailand; Department of Biomedical Sciences, College of Life and Health Sciences, Chubu University, Aichi, Japan.
authors.forename: Nongluk
authors.initials: N
authors.lastname: Sriwilaijaroen
authors.affiliation: Cancer Glycosylation Research, Institute of Molecular Biomembrane and Glycobiology, Tohoku Pharmaceutical University, Sendai, Japan.
authors.forename: Setsuko
authors.initials: S
authors.lastname: Moriya
authors.affiliation: Department of Applied Bioorganic Chemistry, Faculty of Applied Biological Sciences, Gifu University, Gifu, Japan.
authors.forename: Hiromune
authors.initials: H
authors.lastname: Ando
authors.affiliation: Cancer Glycosylation Research, Institute of Molecular Biomembrane and Glycobiology, Tohoku Pharmaceutical University, Sendai, Japan.
authors.forename: Taeko
authors.initials: T
authors.lastname: Miyagi
authors.affiliation: Department of Biomedical Sciences, College of Life and Health Sciences, Chubu University, Aichi, Japan.
authors.forename: Yasuo
authors.initials: Y
authors.lastname: Suzuki
authors.affiliation: Department of Applied Bioorganic Chemistry, Faculty of Applied Biological Sciences, Gifu University, Gifu, Japan.
authors.forename: Hideharu
authors.initials: H
authors.lastname: Ishida
authors.affiliation: Department of Applied Bioorganic Chemistry, Faculty of Applied Biological Sciences, Gifu University, Gifu, Japan; Institute for Integrated Cell-Material Sciences (iCeMS), Kyoto University, Japan.
authors.forename: Makoto
authors.initials: M
authors.lastname: Kiso