Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.

Cowart M; bbott.com; Lee CH; Gfesser GA; Bayburt EK; Bhagwat SS; Stewart AO; Yu H; Kohlhaas KL; McGaraughty S; Wismer CT; Mikusa J; Zhu C; Alexander KM; Jarvis MF; Kowaluk EA

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Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.

机译：5-取代的嘧啶嘧啶作为腺苷激酶抑制剂的结构活性研究。

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The synthesis and SAR of a novel series of non-nucleoside pyridopyrimidine inhibitors of the enzyme adenosine kinase (AK) are described. It was found that pyridopyrimidines with a broad range of medium and large non-polar substituents at the 5-position potently inhibited AK activity. A narrower range of analogues was capable of potently inhibiting adenosine phosphorylation in intact cells indicating an enhanced ability of these analogues to penetrate cell membranes. Potent AK inhibitors were found to effectively reduce nociception in animal models of thermal hyperalgesia and persistent pain.

机译：描述了一系列新型的腺苷激酶（AK）的非核苷嘧啶嘧啶抑制剂的合成和SAR。发现在5-位具有广泛范围的中等和大的非极性取代基的吡啶并嘧啶有效抑制AK活性。较窄范围的类似物能够有效抑制完整细胞中的腺苷磷酸化，表明这些类似物穿透细胞膜的能力增强。在热痛觉过敏和持续性疼痛的动物模型中，发现有效的AK抑制剂可有效减少伤害感受。

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《Bioorganic and Medicinal Chemistry Letters》 |2001年第1期|共4页
作者
Cowart M; bbott.com; Lee CH; Gfesser GA; Bayburt EK; Bhagwat SS; Stewart AO; Yu H; Kohlhaas KL; McGaraughty S; Wismer CT; Mikusa J; Zhu C; Alexander KM; Jarvis MF; Kowaluk EA;
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正文语种 eng
中图分类药学;生物化学;
关键词
Adenosine Kinase; Enzyme Inhibitors; Pyrimidines; 腺苷激酶; 酶抑制剂; 嘧啶类;

机译：Adenosine Kinase;Enzyme Inhibitors;Pyrimidines;腺苷激酶;酶抑制剂;嘧啶类;

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1. Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors. [J] . Cowart M, bbott.com, Lee CH, Bioorganic and Medicinal Chemistry Letters . 2001,第1期

机译：5-取代的嘧啶嘧啶作为腺苷激酶抑制剂的结构活性研究。
2. Pyridopyrimidine analogues as novel adenosine kinase inhibitors. [J] . Zheng GZ, bbott.com, Lee C, Bioorganic and Medicinal Chemistry Letters . 2001,第16期

机译：吡啶并嘧啶类似物作为新型腺苷激酶抑制剂。
3. 4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors. [J] . Matulenko MA, Paight ES, Frey RR, Bioorganic and medicinal chemistry . 2007,第4期

机译：4-氨基-5-芳基-6-芳基乙炔基嘧啶：非核苷腺苷激酶抑制剂的结构活性关系。
4. Adenosine monophosphate-activated protein kinase status modulates kinetics of post-mortem pH decline and meat quality in pig Longissimus muscle [C] . Faure J., Lebret B., Ecolan P., ICoMST 2011;International conference of meat science and technology . 2012

机译：腺苷一磷酸激活的蛋白激酶状态调节猪Longissimus肌肉的死后pH下降和肉质动力学
5. Part I. The synthesis and structure-activity relationship study of azo dye related HIV replication inhibitors. Part II. Plant isolation of signalling pathways inhibitors as anti-cancer agents. [D] . Lu, Hang. 1994

机译：第一部分：偶氮染料相关的HIV复制抑制剂的合成及其构效关系研究。第二部分植物分离的信号通路抑制剂为抗癌剂。
6. Structure-activity relationship for adenosine kinase from Mycobacterium tuberculosis [O] . Mary C. Long, Sue C. Shaddix, Omar Moukha-Chafiq, -1

机译：结核分枝杆菌腺苷激酶的构效关系
7. Adenosine Kinase Inhibitors. 6. Synthesis, Water Solubility, and Antinociceptive Activity of 5-Phenyl-7-(5-deoxy-b-d-ribofuranosyl)pyrrolo2, 3-dpyrimidines Substituted at C4 with Glycinamides and Related Compounds [O] . -1

机译：腺苷激酶抑制剂。 6.用糖酰胺和相关化合物取代的5-苯基-7-（5-脱氧-7-（5-脱氧-B-D-核糖基）吡咯并2,3-d嘧啶的合成，水溶性和抗血质活性
8. Levels of Adenosine Deaminase, AMP Deaminase, and Adenylate Kinase in Cultured Human Lymphoblast Lines: Exquisite Sensitivity of AMP Deaminase to Adenosine Deaminase Inhibitors. [R] . Fishbein, W. N., Davis, J. I., Winkert, J. W., 1981

机译：培养的人淋巴母细胞系中腺苷脱氨酶，amp脱氨酶和腺苷酸激酶的水平：amp脱氨酶对腺苷脱氨酶抑制剂的精确敏感性。

Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.

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