171663-06-2Relevant articles and documents
First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate
Cinelli, Maris A.,Reidl, Cory T.,Li, Huiying,Chreifi, Georges,Poulos, Thomas L.,Silverman, Richard B.
, p. 4528 - 4554 (2020/05/05)
Inhibition of neuronal nitric oxide synthase (nNOS), an enzyme implicated in neurodegenerative disorders, is an attractive strategy for treating or preventing these diseases. We previously developed several classes of 2-aminoquinoline-based nNOS inhibitor
Palladium-Catalyzed C(sp2)-H Olefination of Free Primary and Secondary 2-Phenylethylamines: Access to Tetrahydroisoquinolines
Fan, Shuai,Ding, Yongzheng,Chen, Xiaoxi,Gao, Yuzhen,Fu, Lei,Li, Shangda,Li, Gang
, p. 13003 - 13012 (2019/10/11)
A rapid construction of THIQs by a Pd(II)-catalyzed C(sp2)-H olefination of free primary and secondary 2-phenylethylamines with high step- and atom-economy was reported. Notably, no substituent was required at the α-position to the amino group of the 2-phenylethylamines. The substrate scope was broad, and the reaction could also be applied to generate THIQs from the biologically active molecules such as the drug molecule baclofen and phenylalanine ester.
Phenethyl nicotinamides, a novel class of NaV1.7 channel blockers: Structure and activity relationship
Kers, Inger,MacSari, Istvan,Csjernyik, Gabor,Nyloef, Martin,Skogholm, Karin,Sandberg, Lars,Minidis, Alexander,Bueters, Tjerk,Malmborg, Jonas,Eriksson, Anders B.,Lund, Per-Eric,Venyike, Elisabet,Luo, Lei,Nystroem, Jan-Erik,Besidski, Yevgeni
, p. 6108 - 6115 (2012/10/30)
The NaV1.7 ion channel is an attractive target for development of potential analgesic drugs based on strong genetic links between mutations in the gene coding for the channel protein and inheritable pain conditions. The (S)-N-chroman-3-ylcarboxamide series, exemplified by 1, was used as a starting point for development of new channel blockers, resulting in the phenethyl nicotinamide series. The structure and activity relationship for this series was established and the metabolic issues of early analogues were addressed by appropriate substitutions. Compound 33 displayed acceptable overall in vitro properties and in vivo rat PK profile.