|標題:||Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities|
von Itzstein, Mark
Mong, Kwok Kong T.
Department of Biological Science and Technology
Department of Applied Chemistry
|摘要:||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.|
|期刊:||ORGANIC & BIOMOLECULAR CHEMISTRY|