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ID: ALA1136699

Journal: Bioorg Med Chem Lett

Title: Discovery and SAR of novel Naphthyridines as potent inhibitors of spleen tyrosine kinase (SYK).

Authors: Cywin CL, Zhao BP, McNeil DW, Hrapchak M, Prokopowicz AS, Goldberg DR, Morwick TM, Gao A, Jakes S, Kashem M, Magolda RL, Soll RM, Player MR, Bobko MA, Rinker J, DesJarlais RL, Winters MP.

Abstract: 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.

CiteXplore: 12668002

DOI: 10.1016/s0960-894x(03)00163-x