A series of novel pyrazole fused heterocyclic derivatives were synthesized via a two-step procedure or a one-pot two step method, and their catalytic DNA cleavage abilities and anti-BVDV activities were also evaluated...A series of novel pyrazole fused heterocyclic derivatives were synthesized via a two-step procedure or a one-pot two step method, and their catalytic DNA cleavage abilities and anti-BVDV activities were also evaluated. The results obtained indicated that compounds 3b-3c could catalyze the cleavage of supercoiled DNA （pUC 19 plasmid DNA） to nicked DNA under physiological conditions with high yields via a hydrolytic mechanism. The studies on anti-viral activities against bovine viral diarrhea virus （BVDV） demonstrated that some of the pyrazole derivatives showed pronounced anti-BVDV activity with interesting ECso values and no significant cytotoxicity. Among them, compound 31 showed the highest antiviral activity （ECso = 0.12 μmol/L） and was 10 fold more than that of the positive control ribavirin （ECso = 1.3 μmol/L）, which provided a potential candidate for the development of anti-BVDV agents.展开更多
基金the National Natural Science Foundation of China (Nos.21105091 and 20772113) for the financial support
文摘A series of novel pyrazole fused heterocyclic derivatives were synthesized via a two-step procedure or a one-pot two step method, and their catalytic DNA cleavage abilities and anti-BVDV activities were also evaluated. The results obtained indicated that compounds 3b-3c could catalyze the cleavage of supercoiled DNA （pUC 19 plasmid DNA） to nicked DNA under physiological conditions with high yields via a hydrolytic mechanism. The studies on anti-viral activities against bovine viral diarrhea virus （BVDV） demonstrated that some of the pyrazole derivatives showed pronounced anti-BVDV activity with interesting ECso values and no significant cytotoxicity. Among them, compound 31 showed the highest antiviral activity （ECso = 0.12 μmol/L） and was 10 fold more than that of the positive control ribavirin （ECso = 1.3 μmol/L）, which provided a potential candidate for the development of anti-BVDV agents.
