Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors

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• 作者：Fernando Padilla ; Niala Bhagirath ; Shaoqing Chen ; Eric Chiao ; David M. Goldstein ; Johannes C. Hermann ; Jonathan Hsu ; Joshua J. Kennedy-Smith ; Andreas Kuglstatter ; Cheng Liao ; Wenjian Liu ; Lee E. Lowrie ; Jr. ; Kin Chun Luk ; Stephen M. Lynch ; John Menke ; Linghao Niu ; Timothy D. Owens ; Counde O-Yang ; Aruna Railkar ; Ryan C. Schoenfeld ; Michelle Slade ; Sandra Steiner ; Yun-Chou Tan ; Armando G. Villase帽or ; Ce Wang ; Jutta Wanner ; Wenwei Xie ; Daigen Xu ; Xiaohu Zhang ; Mingyan Zhou ; Matthew C. Lucas
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：February 28, 2013
• 年：2013
• 卷：56
• 期：4
• 页码：1677-1692
• 全文大小：751K
• 年卷期：v.56,no.4(February 28, 2013)
• ISSN：1520-4804

文摘

We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in physicochemical properties and human whole blood potencies. Ultimately, our mouse model revealed unexpected toxicity that precluded us from further advancing this series.