The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors
Leucine-rich repeat kinase 2 (LRRK2) has attracted considerable interest as a therapeutic target for the treatment of Parkinson's disease. Compounds derived from a 2-aminopyridine screening hit were optimised using a LRRK2 homology model based on mixed li
Smith, Garrick P.,Badolo, Lassina,Chell, Victoria,Chen, I-Jen,Christensen, Kenneth Vielsted,David, Laurent,Daechsel, Justus Alfred,Hentzer, Morten,Herzig, Martin Christian,Mikkelsen, Gitte Kobber?e,Watson, Stephen P.,Williamson, Douglas S.
p. 4500 - 4505
(2017/09/12)
False positives in a reporter gene assay: Identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase
Luciferase reporter-gene assays are a commonly used technique in high-throughput screening campaigns. In this study, we report on a luciferase inhibitor (1), which emerged from an antagonistic G protein-coupled receptor luciferase reporter-gene assay scre
Heitman, Laura H.,Van Veldhoven, Jacobus P. D.,Zweemer, Annelien M.,Ye, Kai,Brussee, Johannes,Ijzerrnan, Adriaan P.
supporting information; experimental part
p. 4724 - 4729
(2009/06/18)
A new class of pyrazolopyridine nucleus with fluorescent properties, obtained through either a radical or a Pd arylation pathway from N-azinylpyridinium N-aminides
(Chemical Equation Presented) The synthesis of dipyridopyrazole and pyridopyrazolopyrazine derivatives - both of which incorporate a 3-aryl moiety - can be achieved in moderate yields by intramolecular radical arylation of pyridinium N-aminides using tris(trimethylsilyl)silane and azobisisobutyronitrile. Improved results were obtained on using Pd direct arylation in conjunction with microwave irradiation. A preliminary study into the fluorescent properties of the target compounds is also reported.
Abet, Valentina,Nunez, Araceli,Mendicuti, Francisco,Burgos, Carolina,Alvarez-Builla, Julio
scheme or table
p. 8800 - 8807
(2009/04/11)
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