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C. Han et al. / Chinese Chemical Letters xxx (2015) xxx–xxx
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Compound
R1
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3a
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254
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value of 0.12–0.25
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Preliminary SAR showed that different substitution at the
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compounds 3a–3d), showed no remarkable antiviral activities,
indicating an importance of the pyrazole N-substitution. When
replacing the N-hydrogen atom by phenyl group, their antiviral
activities were obviously improved (Table 1, compounds 3e–3h).
Especially, while different substituted phenyls were introduced to
the pyrazole N, where the substituent on the lactam N (R1) is
unsubstituted phenyl, their antiviral activities were further
improved (Table 1, compounds 3i–3l). Compound 3l (R1 = Ph,
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268
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In conclusion, we have successfully synthesized a series of novel
pyrazole fused heterocyclic derivatives via a two-step procedure or
a one-pot two step strategy, and investigated their catalytic DNA
cleavage abilities and anti-BVDV activities. With 3b–3c, the plasmid
DNA could be cleaved from Form I to Form II completely via a
hydrolytic mechanism under mild conditions in a short time.
Meanwhile, most of the tested compounds exhibited excellent anti
rivalactivitiesagainstBVDVwithnosignificantcytotoxicity. Among
them, compound 3l showed the highest antiviral activity
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Acknowledgment
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282 Q3
We thank the National Natural Science Foundation of China
(Nos. 21105091 and 20772113) for the financial support.
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Please cite this article in press as: C. Han, et al., Novel pyrazole fused heterocyclic ligands: Synthesis, characterization, DNA binding/