College of Chemistry & Pharmacy, Shaanxi Key Laboratory of Natural Products & Chemical Biology, Northwest A&F University, Yangling, Shaanxi 712100, PR China.
Key Laboratory of Botanical Pesticide R&D in Shaanxi Province, Yangling, Shaanxi 712100, PR China.
Bioorg Med Chem. 2018 Sep 1;26(16):4644-4649. doi: 10.1016/j.bmc.2018.07.041. Epub 2018 Jul 25.
A series of l-pyroglutamic acid analogues from natural product lead were designed and synthesized, as well as their antifungal activities against Phytophthora infestans, neuritogenic activities, antibacterial activities and anti-inflammatory activities are described. The bioassays and SAR study showed that the majority of l-pyroglutamic acid esters have a significant antifungal activity against P. infestans, especially 2d and 2j demonstrated the best activities with EC values of 1.44 and 1.21 μg mL, which were about seven times that of commercial azoxystrobin (7.85 μg mL). Moreover, compounds 2e, 2g and 4d displayed anti-inflammatory activity against LPS-induced NO production in BV-2 microglial cells; neuritogenic activity in NGF-induced PC-12 cells is the same activity. This study demonstrates that compounds 2d and 2j are potential drugs to control P. infestans.
从天然产物先导物中设计并合成了一系列 l-焦谷氨酸类似物，并对其进行了抗疫霉属真菌活性、促神经突生成活性、抗菌活性和抗炎活性的描述。生物测定和 SAR 研究表明，大多数 l-焦谷氨酸酯类化合物对疫霉属真菌具有显著的抗真菌活性，特别是 2d 和 2j 表现出最佳活性，EC 值分别为 1.44 和 1.21μg/mL，约为商业制剂唑菌胺酯（7.85μg/mL）的七倍。此外，化合物 2e、2g 和 4d 对 LPS 诱导的 BV-2 小胶质细胞中 NO 产生具有抗炎活性；在 NGF 诱导的 PC-12 细胞中具有促神经突生成活性。本研究表明，化合物 2d 和 2j 是潜在的防治疫霉属真菌的药物。
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