期刊
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
卷 62, 期 5, 页码 1010-1018出版社
AMER CHEMICAL SOC
DOI: 10.1021/jf404840x
关键词
beta-carboline; dihydro-beta-carboline; tetrahydro-beta-carboline; alkaloids; anti-TMV; fungicidal activity; structure-activity relationship
资金
- National Key Project for Basic Research [2010CB126106]
- National Natural Science Foundation of China [21132003, 21121002, 21372131]
- Specialized Research Fund for the Doctoral Program of Higher Education [20130031110017]
Six known beta-carboline, dihydro-beta-carboline, and tetrahydro-beta-carboline alkaloids and a series of their derivatives were designed, synthesized, and evaluated for their anti-tobacco mosaic virus (TMV) and fungicidal activities for the first time. All of the alkaloids and some of their derivatives (compounds 3, 4, 14, and 19) exhibited higher anti-TMV activity than the commercial antiviral agent Ribavirin both in vitro and in vivo. Especially, the inactivation, curative, and protection activities of alkaloids Harmalan (62.3, 55.1, and 60.3% at 500 mu g/mL) and tetrahydroharmane (64.2, 57.2, and 59.5% at 500 mu g/mL) in vivo were much higher than those of Ribavirin (37.4, 36.2, and 38.5% at 500 mu g/mL). A new derivative, 14, with optimized physicochemical properties, obviously exhibited higher activities in vivo (50.4, 43.9, and 47.9% at 500 mu g/mL) than Ribavirin and other derivatives; therefore, 14 can be used as a new lead structure for the development of anti-TMV drugs. Moreover, most of these compounds exhibited good fungicidal activity against 14 kinds of fungi, especially compounds 4, 7, and 11.
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