852402-70-1Relevant articles and documents
HCV NS5A replication complex inhibitors. Part 4.1 optimization for genotype 1a replicon inhibitory activity
St. Laurent, Denis R.,Serrano-Wu, Michael H.,Belema, Makonen,Ding, Min,Fang, Hua,Gao, Min,Goodrich, Jason T.,Krause, Rudolph G.,Lemm, Julie A.,Liu, Mengping,Lopez, Omar D.,Nguyen, Van N.,Nower, Peter T.,O'Boyle, Donald R.,Pearce, Bradley C.,Romine, Jeffrey L.,Valera, Lourdes,Sun, Jin-Hua,Wang, Ying-Kai,Yang, Fukang,Yang, Xuejie,Meanwell, Nicholas A.,Snyder, Lawrence B.
, p. 1976 - 1994 (2014/04/03)
A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity against BVDV and cytotoxicity. SAR emerging f
Enantiomerically pure hexahydropyrazinoquinolines as potent and selective dopamine 3 subtype receptor ligands
Ding, Ke,Chen, Jianyong,Ji, Min,Wu, Xihan,Varady, Judith,Yang, Chao-Yie,Lu, Yipin,Deschamps, Jeffrey R.,Levant, Beth,Wang, Shaomeng
, p. 3171 - 3181 (2007/10/03)
We report the design and synthesis of a series of enantiomerically pure hexahydropyrazinoquinolines as potent and selective ligands for the dopamine 3 subtype receptor using a newly developed synthetic method and using in vitro pharmacological evaluation. Our efforts yielded optically pure ligands with high affinities for the D3 receptor and outstanding selectivity over closely related D1-like and D2-like receptors. For example, compound 38a has a Ki value of 5.7 nM to the D3 receptor and selectivity greater than 10000- and 1600-fold over the D 1-like and D2-like receptors, respectively, and thus is one of the most selective D3 ligands reported to date.
