含磺酸酯部分的新型辣椒素衍生物的合成、抗菌及杀虫活性
Synthesis, Antibacterial and Insecticidal Activities of Novel Capsaicin Derivatives Containing a Sulfonic Acid Esters Moiety.
作者信息
Xie Dandan, Yang Zaiping, Hu Xin, Wen Yin
机构信息
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, China.
School of Biology and Engineering, Guizhou Medical University, Guiyang, China.
出版信息
Front Chem. 2022 Jun 14;10:929050. doi: 10.3389/fchem.2022.929050. eCollection 2022.
In order to develop an efficient and broad-spectrum bactericide, a series of novel capsaicin derivatives containing a sulfonic acid esters moiety was synthesized. The structure of these compounds were confirmed by nuclear magnetic resonance spectroscopy (NMR) and high-resolution mass spectrum (HRMS). The results of the bioactivities revealed that some target compounds exhibited remarkable antibacterial activity. Compound exhibited the highest activities against pv. (Psa), pv. (Xoo), and pv. (Xac), and the values were 86, 54, and 92% at 50 μg/ml, respectively, which were higher than were for thiodiazole copper (87, 34, and 77%) and bismerthiazol (87, 37 and 75%). Although some compounds also showed certain activity against , it was weaker than the positive controls monosultap and mulfoxaflor. Thus, the bioassay results recommend that these newly designed and synthesized scaffolds should be used as a bactericide lead compound rather than an insecticide lead compound.
为了开发一种高效广谱的杀菌剂，合成了一系列含有磺酸酯部分的新型辣椒素衍生物。通过核磁共振光谱（NMR）和高分辨率质谱（HRMS）确认了这些化合物的结构。生物活性结果表明，一些目标化合物表现出显著的抗菌活性。化合物对丁香假单胞菌番茄致病变种（Psa）、水稻白叶枯病菌（Xoo）和柑橘溃疡病菌（Xac）表现出最高活性，在50μg/ml时的值分别为86%、54%和92%，高于噻菌铜（87%、34%和77%）和叶枯唑（87%、37%和75%）。虽然一些化合物对也表现出一定活性，但比阳性对照杀螟丹和氯虫·氟氯氰菊酯弱。因此，生物测定结果表明，这些新设计合成的支架应作为杀菌剂先导化合物而非杀虫剂先导化合物。
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