title: Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities.
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 , with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.
authors.affiliation: Department of Chemistry, National Tsing Hua University, 101, Section 2, Kuang-Fu Road, Hsinchu 30013, Taiwan.
authors.forename: Chien-Hung
authors.initials: CH
authors.lastname: Lin
authors.forename: Tsung-Che
authors.initials: TC
authors.lastname: Chang
authors.forename: Anindya
authors.initials: A
authors.lastname: Das
authors.forename: Ming-Yu
authors.initials: MY
authors.lastname: Fang
authors.forename: Hui-Chen
authors.initials: HC
authors.lastname: Hung
authors.forename: Kai-Cheng
authors.initials: KC
authors.lastname: Hsu
authors.forename: Jinn-Moon
authors.initials: JM
authors.lastname: Yang
authors.forename: Mark
authors.initials: M
authors.lastname: von Itzstein
authors.forename: Kwok Kong T
authors.initials: KK
authors.lastname: Mong
authors.forename: Tsu-An
authors.initials: TA
authors.lastname: Hsu
authors.forename: Chun-Cheng
authors.initials: CC
authors.lastname: Lin
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019791:Guanidine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects; D053122:Influenza A Virus, H3N2 Subtype / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D053243:Zanamivir / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D009439:Neuraminidase; D019791:Guanidine; D053243:Zanamivir