Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
Basic Information
ID: ALA4229537
Journal: Bioorg Med Chem
Title: Synthesis and bioactivities evaluation of l-pyroglutamic acid analogues from natural product lead.
Authors: Gang FL, Zhu F, Li XT, Wei JL, Wu WJ, Zhang JW.
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.
CiteXplore: 30119995
DOI: 10.1016/j.bmc.2018.07.041
Patent ID: ┄