Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

…, KC Hsu, JM Yang, M Von Itzstein, KKT Mong…

Index: Lin, Chien-Hung; Chang, Tsung-Che; Das, Anindya; Fang, Ming-Yu; Hung, Hui-Chen; Hsu, Kai-Cheng; Yang, Jinn-Moon; Von Itzstein, Mark; Mong, Kwok Kong T.; Hsu, Tsu-An; Lin, Chun-Cheng Organic and Biomolecular Chemistry, 2013 , vol. 11, # 24 p. 3943 - 3948

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Citation Number: 13

Abstract

A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.