2. Academic Validation
  3. Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead

Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead

  • Bioorg Med Chem. 2018 Sep 1;26(16):4644-4649. doi: 10.1016/j.bmc.2018.07.041.
Fang-Li Gang 1,  Feng Zhu 1,  Xiao-Ting Li 1,  Jie-Lu Wei 1,  Wen-Jun Wu 2,  Ji-Wen Zhang 3
Affiliations

Affiliations

  • 1 College of Chemistry & Pharmacy, Shaanxi Key Laboratory of Natural Products & Chemical Biology, Northwest A&F University, Yangling, Shaanxi 712100, PR China.
  • 2 Key Laboratory of Botanical Pesticide R&D in Shaanxi Province, Yangling, Shaanxi 712100, PR China.
  • 3 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. Electronic address: nwzjw@nwafu.edu.cn.
PMID: 30119995 DOI: 10.1016/j.bmc.2018.07.041
Abstract

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 EC50 values of 1.44 and 1.21 μg mL-1, which were about seven times that of commercial azoxystrobin (7.85 μg mL-1). 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.

Keywords

Anti-inflammatory activity; Antifungal activity; Neuritogenic activity; Structure-activity-relationship; l-Pyroglutamic acid.

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