461400-41-9Relevant articles and documents
Metal-Free C–S Bond Cleavage to Access N-Substituted Acrylamide and β-Aminopropanamide
Yang, Ke,Li, Yi,Ma, Zhiyan,Tang, Long,Yin, Yue,Zhang, Hao,Li, Zhengyi,Sun, Xiaoqiang
, p. 5812 - 5814 (2019)
Metal-free and Selectfluor-mediated C–S bond cleavage is described. This novel strategy provides a facile and efficient method to access important N-substituted acrylamide and β-aminopropanamide derivatives with good functional group tolerance and yields.
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333
Beinat, Corinne,Banister, Samuel D.,Van Prehn, Saundra,Doddareddy, Munikumar Reddy,Hibbs, David,Sako, Michael,Chebib, Mary,Tran, Thao,Al-Muhtasib, Nour,Xiao, Yingxian,Kassiou, Michael
supporting information; experimental part, p. 2380 - 2384 (2012/05/05)
A series of ligands based on SEN12333, containing either contracted or elongated alkyl chains, were synthesized and evaluated in molecular docking studies against a homology model of the α7 nicotinic acetylcholine receptor (nAChR) subtype. The predicted binding of all ligands was highly similar, with the exception of the analog containing a 5 methylene unit spacer. However, in vitro competition binding assays revealed that the ligands possessed dissimilar binding affinities, with a Ki range of more than an order of magnitude (Ki = 0.50 to >10 μM), and only SEN12333 itself exhibited functional activity at the α7 nAChR.
