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Synthesis and antiviral evaluation of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates.

Abstract：

:A series of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates were synthesized and their in vitro and in vivo antiviral activities were evaluated via microscale thermophoresis method and half-leaf method, respectively. The in vitro results indicated that compounds 7g, 7l, 8h, and 8l displayed good antiviral activity against TMV, with the binding constant values of 5.93, 6.15, 6.02, and 5.04μM, respectively, which were comparable to that of Ninnanmycin (6.78μM) and even better than that of Ribavirin (99.25μM). The in vivo results demonstrated that compounds 7g, 7l, 8h, and 8l exhibited remarkable anti-TMV activity with the EC50 values of 33.66, 33.97, 33.87 and 30.57µg/mL, respectively, which were comparable to that of Ningnanmycin (36.85µg/mL) and superior to that of Ribavirin (88.52µg/mL). Interestingly, the trend of antiviral activity in vivo was consistent with the in vitro results.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gan X,Hu D,Chen Z,Wang Y,Song B

doi

10.1016/j.bmcl.2017.08.038

subject

Has Abstract

pub_date

2017-09-15 00:00:00

pages

4298-4301

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(17)30839-9

journal_volume

27

pub_type

杂志文章

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