Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors [electronic resource]

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Tác giả:

Ngôn ngữ: eng

Ký hiệu phân loại: 547.2 Organic chemical reactions formerly 547.139

Thông tin xuất bản: Argonne, Ill. : Oak Ridge, Tenn. : Argonne National Laboratory ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2015

Mô tả vật lý: Size: p. 942-947 : , digital, PDF file.

Bộ sưu tập: Metadata

ID: 261175

 We report the identification and synthesis of a series of aminopyrimidin-4-one IRAK4 inhibitors. Through high throughput screening, an aminopyrimidine hit was identified and modified via structure enabled design to generate a new, potent, and kinase selective pyrimidin-4-one chemotype. This chemotype is exemplified by compound 16, which has potent IRAK4 inhibition activity (IC<
 sub>
 50<
 /sub>
  = 27 nM) and excellent kinase selectivity (>
 100-fold against 99% of 111 tested kinases), and compound 31, which displays potent IRAK4 activity (IC<
 sub>
 50<
 /sub>
  = 93 nM) and good rat bioavailability (F = 42%).
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