Inhibitory effect and structure–activity relationship of some Biginelli-type pyrimidines against HSV-1

摘要: Inevitable emergence of multi-drug resistant strains to current available drugs makes an impetus for finding new therapeutic agents against herpes simplex virus (HSV). In this study, a series novel derivatives Biginelli-type pyrimidines were evaluated as potential anti-HSV-1 compounds by plaque reduction method. The cellular toxicity was assessed XTT proliferation assay. time course anti-HSV activity the most active compound studied show anti-viral effect in various intervals replication cycle. Compounds 2, 6, 8, 11, 12, 17, 18, 20, and 40 had highest inhibition HSV. Compound inhibited HSV with IC50 0.9 μmol/l CC50 up 100 μmol/l. This noteworthy inhibitor TI value 111. 20 also showed considerable inhibitory 1.8 Result time-of-addition study that inhibits at stage after entry virions target cells. Analysis structure demonstrated clear relationships their effects. Some seem be promising candidates future drug discovery researches. Structural manipulation based on obtained structure–activity would propose some leads programs.