Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

Shook BC; Rassnick S; Hall D; Rupert KC; Heintzelman GR; Hansen K; Chakravarty D; Bullington JL; Scannevin RH; Magliaro B; Westover L; Carroll K; Lampron L; Russell R; Branum S; Wells K; Damon S; Youells S; Li X; Osbourne M; Demarest K; Tang Y; Rhodes K; Jackson PF

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

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Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

机译：亚甲基胺取代的arylindenopyrimidines作为有效的腺苷A（2A）/ A（1）拮抗剂。

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A novel series of arylindenopyrimidines were identified as A(2A) and A(1) receptor antagonists. The series was optimized for in vitro activity by substituting the 8- and 9-positions with methylene amine substituents. The compounds show excellent activity in mouse models of Parkinson's disease when dosed orally.

机译：一系列新的arylindenopyrimidines被确定为A（2A）和A（1）受体拮抗剂。通过用亚甲基胺取代基取代8位和9位，优化了该系列的体外活性。当口服给药时，该化合物在帕金森氏病小鼠模型中显示出色的活性。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第9期|共4页
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Shook BC; Rassnick S; Hall D; Rupert KC; Heintzelman GR; Hansen K; Chakravarty D; Bullington JL; Scannevin RH; Magliaro B; Westover L; Carroll K; Lampron L; Russell R; Branum S; Wells K; Damon S; Youells S; Li X; Osbourne M; Demarest K; Tang Y; Rhodes K; Jackson PF;
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1. Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists. [J] . Shook BC, Rassnick S, Hall D, Bioorganic and Medicinal Chemistry Letters . 2010,第9期

机译：亚甲基胺取代的arylindenopyrimidines作为有效的腺苷A（2A）/ A（1）拮抗剂。
2. Overcoming the Genotoxicity of a Pyrrolidine Substituted Arylindenopyrimidine As a Potent Dual Adenosine A(2A)/A(1) Antagonist by Minimizing Bioactivation to an Iminium Ion Reactive Intermediate. [J] . Lim HK, Chen J, Sensenhauser C, Chemical research in toxicology . 2011,第7期

机译：通过最大限度地减少对Iminium离子活性中间体的生物活化作用，克服吡咯烷取代的Arylindenopyrimidine作为强力双重腺苷A（2A）/ A（1）拮抗剂的遗传毒性。
3. The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A(2A) Receptor Subtype [J] . Falsini Matteo, Squarcialupi Lucia, Catarzi Daniela, Journal of Medicinal Chemistry . 2017,第13期

机译：1,2,4-三唑唑[4,3-A]吡嗪-3-作为一种多功能支架，用于设计有效的腺苷人受体拮抗剂。靶向A（2A）受体亚型的结构研究
4. Quantitative FRET measurement of the interaction of A_1 adenosine receptors and A_(2A) adenosine receptors in living cell [C] . Yating Lin, Yimei Huang, Zhiwei Wu, Optics in health care and biomedical optics VIII . 2018

机译：活细胞中A_1腺苷受体和A_（2A）腺苷受体相互作用的定量FRET测量
5. Effects of pharmacological inactivation of adenosine 2A receptors in a murine model of polymicrobial sepsis. [D] . Helbig, Brian J. 2016

机译：腺苷2A受体在药理学上的失活在小鼠脓毒症模型中的作用。
6. Novel substituted (Z)-5-((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-24-diones and 5-((N-benzyl-1H-indol-3-yl)methylene)pyrimidine-246(1H3H5H)-triones as potent radio-sensitizing agents [O] . Y. Thirupathi Reddy, Konjeti R. Sekhar, Nidhish Sasi, -1

机译：新型取代（Z）-5 - （（N-苄基-1H-吲哚-3-基）亚甲基）咪唑烷-24-二乙酯和5-（（N-苄基-1H-吲哚-3-基）亚甲基）嘧啶-246（1H3H5H） - 标纹作为有效的无线电敏化剂
7. Striatal pre- and postsynaptic profile of adenosine A(2A) receptor antagonists. [O] . Marco Orru, Jana Bakešová, Marc Brugarolas, 2011

机译：腺苷a（2a）受体拮抗剂的纹状体前和突触后谱。

Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

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