63438-53-9Relevant academic research and scientific papers
Synthesis and bioactivities evaluation of L-pyroglutamic acid analogues from natural product lead
Gang, Fang-li,Zhu, Feng,Li, Xiao-ting,Wei, Jie-lu,Wu, Wen-jun,Zhang, Ji-wen
, p. 4644 - 4649 (2018/08/21)
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.
Flexible and modular syntheses of enantiopure 5-cis-substituted prolinamines from l-pyroglutamic acid
Prause, Felix,Kaldun, Johannes,Arensmeyer, Benjamin,Wennemann, Benedikt,Fr?hlich, Benjamin,Scharnagel, Dagmar,Breuning, Matthias
supporting information, p. 575 - 586 (2015/02/19)
A wide range (25 examples) of 5-cis-substituted prolinamines is prepared in five to ten steps starting from cheap l-pyroglutamic acid. Three routes, differing mainly in the order of introduction of the substituents at the 5-cis position, the pyrrolidine nitrogen atom, and the exocyclic amino function, are successfully developed.
