期刊
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
卷 23, 期 2, 页码 163-175出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/10286020.2020.1729136
关键词
Cinchonidine; cinchonine; quinine analogues; acyloxy; insecticidal activity
资金
- National Natural Science Foundation of China [U1604105, 31901863]
A free 9-hydroxyl group is not necessary for insecticidal activity; C9-substitution is well tolerated; the configuration of the C8/9 position is crucial for insecticidal activity, with 9S-configuration being optimal.
Endeavor to discover biorational natural products-based insecticides, two series (27) of novel 9R/S-acyloxy derivatives of cinchonidine and cinchonine were prepared and assessed for their insecticidal activity against Mythimna separata in vivo by the leaf-dipping method at 1 mg/mL. Among all the compounds, especially derivatives 6l and 6o exhibited the best insecticidal activity with final mortality rates of 75.0% and 71.4%, respectively. Overall, a free 9-hydroxyl group is not a prerequisite for insecticidal activity and C9-substitution is well tolerated; the configuration of C8/9 position is important for insecticidal activity, and 9S-configuration is optimal; 6'-OCH3 moiety is not necessary, removal of it is also acceptable.
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