期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 64, 期 34, 页码 6508-6516出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.6b02683
关键词
tryptophan; biosynthesis; spirooxindole; acylhydrazone; antiviral activity; fungicidal activity; insecticidal activity
资金
- National Natural Science Foundation of China [21132003, 21421062, 21372131, 21602117]
- Specialized Research Fund for the Doctoral Program of Higher Education [20130031110017]
- Tianjin Natural Science Foundation [16JCZDJC32400]
On the basis of the biosynthesis of alkaloids derived from tryptophan and considering the wide use of spirooxindole in drug molecular design, a series of novel spirooxindole derivatives containing an acylhydrazone moiety were designed, synthesized, and first evaluated for their biological activities. The results of bioassays indicated that the target compounds possessed good activities against tobacco mosaic virus (TMV); especially compound 4, containing a tert-butyl at the benzene ring, exhibited the best antiviral activity in vitro and inactivation, curative, and protection activities in vivo (48.4%, 58 +/- 0.4, 55.2 +/- 2.3, and 49.7 +/- 1.1% at 500 mu g/mL, respectively) compared with ribavirin (38.2, 36.4 +/- 0.2, 37.5 +/- 0.2, and 36.4 +/- 0.1% at 500 mu g/mL, respectively) and harmine (44.6, 40.5 +/- 0.2, 38.6 +/- 0.8, and 42.4 +/- 0.6% at 500 mu g/mL, respectively). At the same time, these compounds exhibited fungicidal activity selectively against certain fungi; most of these derivatives exhibited >60% fungicidal activity against Physalospora piricola at 50 mg/kg. Additionally, compounds 25 and 14 displayed excellent insecticidal activities (60% motality against C. pipiens pallens at 0.25 mg/kg) even at very low concentrations.
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