TY - JOUR
T1 - The discovery of new plant activators and scaffolds with potential induced systemic resistance
T2 - From jasmonic acid to pyrrolidone
AU - Chang, Kang
AU - Shi, Yanxia
AU - Chen, Jianqin
AU - He, Zenghui
AU - Xu, Zheng
AU - Zhao, Zhenjiang
AU - Zhu, Weiping
AU - Li, Honglin
AU - Xu, Yufang
AU - Li, Baoju
AU - Qian, Xuhong
N1 - Publisher Copyright:
© 2016 The Royal Society of Chemistry.
PY - 2016
Y1 - 2016
N2 - Plants can develop multifaceted system resistance as a result of infection with pathogens, insects, and some specific microbes or after treatment with specific chemicals.1 Among them, systemic acquired resistance (SAR) and induced systemic resistance (ISR)2 are the two most important types. To activate them, a large number of chemical inducers have been exploited based on the SA pathway. However, the JA pathway was rarely investigated for new plant activators. In this study, starting from JA and its analogs, based on the molecular three-dimensional shape and pharmacophore similarity comparison (SHAFTS), a new lead compound, pyrrolidone, as a new scaffold of plant activators was predicted and a series of 1-phenyl-5-pyrrolidone-3-carboxylic acid derivatives were designed and synthesized. The bioactivity was evaluated, and most of the compounds showed satisfactory activity; especially, compounds 7-11 showed almost no in vitro activity but excellent efficacy against tested diseases, and the prediction of the virtual screening results was also confirmed, which promoted the application of SHAFTS in the development of pesticides.
AB - Plants can develop multifaceted system resistance as a result of infection with pathogens, insects, and some specific microbes or after treatment with specific chemicals.1 Among them, systemic acquired resistance (SAR) and induced systemic resistance (ISR)2 are the two most important types. To activate them, a large number of chemical inducers have been exploited based on the SA pathway. However, the JA pathway was rarely investigated for new plant activators. In this study, starting from JA and its analogs, based on the molecular three-dimensional shape and pharmacophore similarity comparison (SHAFTS), a new lead compound, pyrrolidone, as a new scaffold of plant activators was predicted and a series of 1-phenyl-5-pyrrolidone-3-carboxylic acid derivatives were designed and synthesized. The bioactivity was evaluated, and most of the compounds showed satisfactory activity; especially, compounds 7-11 showed almost no in vitro activity but excellent efficacy against tested diseases, and the prediction of the virtual screening results was also confirmed, which promoted the application of SHAFTS in the development of pesticides.
UR - https://www.scopus.com/pages/publications/84988019240
U2 - 10.1039/c6md00261g
DO - 10.1039/c6md00261g
M3 - 文章
AN - SCOPUS:84988019240
SN - 2040-2503
VL - 7
SP - 1849
EP - 1857
JO - MedChemComm
JF - MedChemComm
IS - 9
ER -