Evaluation of andrographolide-based analogs derived from Andrographis paniculata against Mythimna separata Walker and Tetranychus cinnabarinus Boisduval |
| |
| Institution: | 1. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China;2. Shanghai Pesticide Research Institute, Shanghai 200032, China;3. Department of Biology and Biochemistry, University of Bath, Claverton Down, Bath BA2 7AY, UK |
| |
| Abstract: | To discover new natural-product-based pesticides, we structurally modified andrographolide, a labdane diterpenoid isolated from Andrographis paniculata, and stereoselectively prepared a series of 12α-(substituted)benzylamino-14-deoxyandrographolide derivatives (I–V). Three-dimensional structures of compounds 3c, 3d, IIIa and IIIb were further determined by single-crystal X-ray diffraction. Compounds IIa (R1 = n-C3H7, R2 = PhCH2) exhibited more promising insecticidal activity against Mythimna separata than toosendanin. Compounds 3a (R1 = H), Ib (R1 = H, R2 = 4-ClPhCH2), and IVa (R1 = 4-ClPh, R2 = PhCH2) showed potent acaricidal activity against Tetranychus cinnabarinus. |
| |
| Keywords: | Andrographolide Secondary metabolite Structural modification Pesticidal activity |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
