57702-49-5Relevant articles and documents
Permeant fluorescent probes visualize the activation of sarm1 and uncover an antineurodegenerative drug candidate
Cai, Yang,Cao, Sheng,Du, Yang,Hou, Yun Nan,Huang, Ke,Lee, Chi-Sing,Lee, Hon Cheung,Li, Wan Hua,Wang, Qian Wen,Wang, Sujing,Xie, Xu Jie,Zhang, Hongmin,Zhao, Yong Juan,Zhao, Zhi Ying,Zhu, Wen Jie
, (2021/06/30)
SARM1 regulates axonal degeneration through its NAD-metabolizing activity and is a drug target for neurodegenerative disorders. We designed and synthesized fluorescent conjugates of styryl derivative with pyridine to serve as substrates of SARM1, which exhibited large red shifts after conversion. With the conjugates, SARM1 activation was visualized in live cells following elevation of endogenous NMN or treatment with a cell-permeant NMN-analog. In neurons, imaging documented mouse SARM1 activation preceded vincristine-induced axonal degeneration by hours. Library screening identified a derivative of nisoldipine (NSDP) as a covalent inhibitor of SARM1 that reacted with the cysteines, especially Cys311 in its ARM domain and blocked its NMN-activation, protecting axons from degeneration. The Cryo-EM structure showed that SARM1 was locked into an inactive conformation by the inhibitor, uncovering a potential neuroprotective mechanism of dihydropyridines.
A novel DMSO-assisted regioselective iodination of aniline analogues
Bovonsombat, Pakorn,Lorpaiboon, Wanutcha,Laoboonchai, Sarocha,Sriprachaya-anunt, Prima,Yimkosol, Warangkana,Siriphatcharachaikul, Natthapatch,Siricharoensang, Pornpawit,Kangwannarakul, Terawee,Maeda, Jin,Losuwanakul, Satreerat,Mahesh Abhyankar, Maitraye
, (2020/10/05)
A metal- and oxidant-free electrophilic iodination of aniline analogues was achieved in high to excellent yields at room temperature in MTBE with 0 or 3.5 equivalents of DMSO. Examined substituents include N-alkyl, N,N-dialkyl, N-morpholinyl and N-piperazinyl as well as methyl, Br, CN and CO2CH3 aryl ring substitutions.
Copper-catalyzed amination of arylboronates with N,N-dialkylhydroxylamines
Matsuda, Naoki,Hirano, Koji,Satoh, Tetsuya,Miura, Masahiro
, p. 3642 - 3645 (2012/05/20)
A tolerant coupling: The title reaction has been developed to deliver arylamines (see scheme; Bz=benzoyl, dppbz=1,2-bis(diphenylphosphino)benzene). The catalysis is based on electrophilic, umpolung amination and enables the use of secondary acyclic amines. Various functional groups are tolerated, thus opening up a new substrate class for the Chan-Lam-type coupling.