125872-67-5Relevant articles and documents
Strong acid-catalyzed electrophilic ring expansion of oxetanes and sulfoxonium ylides
Xie, Wenlai,Xu, Jiaxi,Yuan, Wenhao
, (2021/06/28)
A strong protic acid-catalyzed electrophilic ring expansion of oxetanes into trans-2,3-disubstituted tetrahydrofuran derivatives using sulfoxonium ylides has been developed. This reaction produces functionalized trans-2,3-disubstituted tetrahydrofuran derivatives stereospecifically by using safe and stable sulfoxonium ylides without metal catalysts and the protection of inert gas.
Selective Synthesis of Z-Cinnamyl Ethers and Cinnamyl Alcohols through Visible Light-Promoted Photocatalytic E to Z Isomerization
Li, Hengchao,Chen, Hang,Zhou, Yang,Huang, Jin,Yi, Jundan,Zhao, Hongcai,Wang, Wei,Jing, Linhai
, p. 555 - 559 (2020/02/05)
A photocatalytic E to Z isomerization of alkenes using an iridium photosensitizer under mild reaction conditions is disclosed. This method provides scalable and efficient access to Z-cinnamyl ether and allylic alcohol derivatives in high yields with excellent stereoselectivity. Importantly, this method also provides a powerful strategy for the selective synthesis of Z-magnolol and honokiol derivatives possessing potential biological activity.
Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections
Wei, Hanwen,Mao, Fei,Ni, Shuaishuai,Chen, Feifei,Li, Baoli,Qiu, Xiaoxia,Hu, Linghao,Wang, Manjiong,Zheng, Xinyu,Zhu, Jin,Lan, Lefu,Li, Jian
, p. 235 - 251 (2018/01/17)
Inhibition of S. aureus diapophytoene desaturase (CrtN) could serve as an alternative approach for addressing the tricky antibiotic resistance by blocking the biosynthesis of carotenoid pigment which shields the bacterium from host oxidant killing. In this study, we designed and synthesized 44 derivatives with piperonyl scaffold targeting CrtN and the structure-activity relationships (SARs) were examined extensively to bring out the discovery of 21b with potent efficacy and better hERG safety profile compared to the first class CrtN inhibitor benzocycloalkane derivative 2. Except the excellent pigment inhibitory activity against wild-type S. aureus, 21b also showed excellent pigment inhibition against four pigmented MRSA strains. In addition, H2O2 killing and human whole blood killing assays proved 21b could sensitize S. aureus to be killed under oxidative stress conditions. Notably, the murine study in vivo validated the efficacy of 21b against pigmented S. aureus Newman, vancomycin-intermediate S. aureus Mu50 and linezolid-resistant S. aureus NRS271.