5-amino-pyrazoles as potent and selective p38alpha inhibitors.

Das J; Moquin RV; Dyckman AJ; Li T; Pitt S; Zhang R; Shen DR; McIntyre KW; Gillooly K; Doweyko AM; Newitt JA; Sack JS; Zhang H; Kiefer SE; Kish K; McKinnon M; Barrish JC; Dodd JH; Schieven GL; Leftheris K

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5-amino-pyrazoles as potent and selective p38alpha inhibitors.

机译：5-氨基 - 吡嗪作为有效和选择性P38Alpha抑制剂。

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The synthesis and structure-activity relationships (SAR) of p38alpha MAP kinase inhibitors based on a 5-amino-pyrazole scaffold are described. These studies led to the identification of compound 2j as a potent and selective inhibitor of p38alpha MAP kinase with excellent cellular potency toward the inhibition of TNFalpha production. Compound 2j was highly efficacious in vivo in inhibiting TNFalpha production in an acute murine model of TNFalpha production. X-ray co-crystallography of a 5-amino-pyrazole analog 2f bound to unphosphorylated p38alpha is also disclosed.

机译：描述了基于5-氨基 - 吡唑支架的P38Alpha MAP激酶抑制剂的合成和结构 - 活性关系（SAR）。这些研究导致鉴定化合物2j作为P38Alpha映射激酶的有效和选择性抑制剂，具有优异的细胞效力朝抑制TNFalpha生产。化合物2J在抑制TNFalpha生产的急性小鼠模型中抑制TNFalpha生产的体内高度有效。还公开了5-氨基 - 吡唑类似物2F的X射线共结晶术，其结合到不磷酸化的P38Alpha。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第23期|共4页
作者
Das J; Moquin RV; Dyckman AJ; Li T; Pitt S; Zhang R; Shen DR; McIntyre KW; Gillooly K; Doweyko AM; Newitt JA; Sack JS; Zhang H; Kiefer SE; Kish K; McKinnon M; Barrish JC; Dodd JH; Schieven GL; Leftheris K;
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Bristol-Myers Squibb Research and Development Princeton NJ 08543-4000 USA.;

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正文语种 eng
中图分类药学;
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1. 5-amino-pyrazoles as potent and selective p38alpha inhibitors. [J] . Das J, Moquin RV, Dyckman AJ, Bioorganic and Medicinal Chemistry Letters . 2010,第23期

机译：5-氨基 - 吡嗪作为有效和选择性P38Alpha抑制剂。
2. Piperidine-based heterocyclic oxalyl amides as potent p38alpha MAP kinase inhibitors. [J] . Mavunkel BJ, Perumattam JJ, Tan Bioorganic and Medicinal Chemistry Letters . 2010,第3期

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3. Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors. [J] . Liu H, Kuhn C, Feru F, Bioorganic and Medicinal Chemistry Letters . 2010,第16期

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5-amino-pyrazoles as potent and selective p38alpha inhibitors.

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