Novel β-Cyclodextrin-Based Heptavalent Glycyrrhetinic Acid Conjugates: Synthesis, Characterization, and Anti-Influenza Activity.

ABSTRACT: In our continuing efforts toward the design of novel pentacyclic triterpene derivatives as potential anti-influenza virus entry inhibitors, a series of homogeneous heptavalent glycyrrhetinic acid derivatives based on β-cyclodextrin scaffold were designed and synthesized by click chemistry. The structure was unambiguously characterized by NMR, IR, and MALDI-TOF-MS measurements. Seven conjugates showed sufficient inhibitory activity against influenza virus infection based on the cytopathic effect reduction assay with IC₅₀ values in the micromolar range. The interactions of conjugate 37, the most potent compound (IC₅₀ = 2.86 μM, CC₅₀ > 100 μM), with the influenza virus were investigated using the hemagglutination inhibition assay. M

SUBMITTER: Liang S 

PROVIDER: S-EPMC9039011 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature