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

作者信息

Cywin Charles L, Zhao Bao-Ping, McNeil Daniel W, Hrapchak Matt, Prokopowicz 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

机构信息

Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, CT 06801-0368, USA.

出版信息

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1415-8. doi: 10.1016/s0960-894x(03)00163-x.

DOI:10.1016/s0960-894x(03)00163-x
PMID:12668002
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.

摘要

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