Xiao Junhai

Synthesis and Anti-HBV Activity of Novel Dihydropyrimidine Analogs

Fourteen novel dihydropyrimidine analogs were synthesized from aromatic nitriles through ammonolysis, acetylation, catalytic hydrogenation and cyclization procedures. All the compounds were characterized by 1H NMR, MS and elemental analysis and the antiviral activity was tested in transfected HepG2.2.15 cells. The results show that some compounds had effective activity. The IC50 of compounds 5c and 5n were 0.87 and 0.67 μmol/L, respectively. The structure-activity relationship of 2-heteroaryl was discussed and the interaction of active compounds with capsid was studied by size exclusion chromatography.