562106-01-8Relevant articles and documents
Discovery and SAR of novel [1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK)
Cywin, Charles L.,Zhao, Bao-Ping,McNeil, Daniel W.,Hrapchak, Matt,Prokopowicz III, Anthony S.,Goldberg, Daniel R.,Morwick, Tina M.,Gao, Amy,Jakes, Scott,Kashem, Mohammed,Magolda, Ronald L.,Soll, Richard M.,Player, Mark R.,Bobko, Mark A.,Rinker, James,DesJarlais, Renee L.,Winters, Michael P.
, p. 1415 - 1418 (2007/10/03)
The discovery of novel 5,7-disubstituted[1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK) is discussed. The SAR reveals the necessity for a 7-aryl group with preference towards para substitution and that this in combination with 5-aminoalkylamino substituents further improved the potency of the compounds. The initial SAR as well as a survey of the other positions is discussed in detail.
