id author title date pages extension mime words sentences flesch summary cache txt cord-340832-412qre64 Liang, Pi‐Hui Novel Five‐Membered Iminocyclitol Derivatives as Selective and Potent Glycosidase Inhibitors: New Structures for Antivirals and Osteoarthritis 2006-01-05 .txt text/plain 3832 221 55 In the screening for 166 www.chembiochem.org a-glucosidase (bakers' yeast) inhibition, about two-thirds of reaction products were found to be more potent than 4 (see Supporting Information for overall library inhibitory activities). With the potent a-glucosidase inhibitors in hand, we tested their potential antiviral effect based on our previous assay system for JEV and DEN-2. [16] The weaker a-glucosidase inhibitors 39-41, derived from core 4 with eight to ten carbons (Scheme 3), were then evaluated, and we found that 39-41 at 10 or 50 mM did not inhibit either JEV or DEN-2 infection (data not shown) in the cell-based assay. The N-alkylated derivatives of compound 24 were also tested for antiviral activity, and 36-38, which contain lipophilic alkyl groups, were the most active, with an IC 50 of about 5-10 mM against JEV, DEN-2, and SARS-CoV infection. However, extending the alkyl chain at the ring nitrogen gave the most potent human b-hexosaminidase inhibitor known to date, that is, compound 54, with a K i value of 2.6 nM. ./cache/cord-340832-412qre64.txt ./txt/cord-340832-412qre64.txt