Evaluation of a Set of C9 N-acyl Neu5Ac2en Mimetics as Viral Sialidase Selective Inhibitors. (8th December 2010)

• Record Type: Journal Article
• Authors: Magesh, Sadagopan; Sriwilaijaroen, Nongluk; Moriya, Setsuko; Ando, Hiromune; Miyagi, Taeko; Suzuki, Yasuo; Ishida, Hideharu; Kiso, Makoto
• Other Names: Rastelli Giulio Academic Editor.
• Is Part Of: International journal of medicinal chemistry. Volume 2011(2011)
• Publication Date: 2010-12-08
• Subjects: Pharmaceutical chemistry -- Periodicals; Chemistry, Pharmaceutical; Pharmaceutical chemistry; Periodicals; 615.19
• DOI: 10.1155/2011/539245
• Languages: English
• ISSNs: 2090-2069

Abstract

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. Compound8 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 compound8 with viral sialidases.