Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.

Beattie D; Brearley A; Brown

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Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.

机译：两系列4'-亚沙 - 碳环核苷作为腺苷A2A受体激动剂的合成与评价。

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The synthesis of two series of 4'-aza-carbocyclic nucleosides are described in which the 4'-substituent is either a reversed amide, relative to the carboxamide of NECA, or an N-bonded heterocycle. Using established purine substitution patterns, potent and selective examples of agonists of the human adenosine A(2A) receptor have been identified from both series. The propionamides 14-18 and the 4-hydroxymethylpyrazole 32 were determined to be the most potent and selective examples from the 4'-reversed amide and 4'-N-bonded heterocyclic series, respectively.

机译：描述了两种系列的4'-甲基碳环核苷的合成，其中4'-取代基相对于NECA的甲酰胺或N键合杂环是反转的酰胺。使用已鉴定的纯化嘌呤替代模式，有效和选择性和选择性的人腺苷A（2A）受体的激动剂的实例已从两种系列中鉴定。将丙酰胺14-18和4-羟甲基吡唑32分别是来自4'-反向酰胺和4'-n键合杂环系的最有效和选择性实例。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共6页
作者
Beattie D; Brearley A; Brown;
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Novartis Institutes for BioMedical Research Respiratory Diseases Area Horsham United Kingdom.;

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正文语种 eng
中图分类药学;生物化学;
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1. Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists. [J] . Beattie D, Brearley A, Brown Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：两系列4'-亚沙 - 碳环核苷作为腺苷A2A受体激动剂的合成与评价。
2. Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists. [J] . Baraldi PG, Cacciari B, Pineda-de-Las-Infantas MJ, Journal of Medicinal Chemistry . 1998,第17期

机译：一系列新的N6-芳基氨基甲酰基，2-（Ar）炔基-N6-芳基氨基甲酰基和N-6羧酰胺基腺苷5'-N-乙基脲酰胺衍生物作为A1和A3腺苷受体激动剂的合成和生物活性。
3. Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. [J] . Devine SM, Gregg A, Figler H, Bioorganic and medicinal chemistry . 2010,第9期

机译：合成和评估作为A3腺苷受体激动剂的新型N6-取代腺苷5'-N-甲基羧酰胺。
4. The selective antagonism of A2A adenosine receptors prevents synaptic failure induced by oxygen and glucose deprivation in rat dentate gyrus [C] . Maraulaa G., Trainia C., Mellob T., European Congress of Pharmacology . 2012

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5. The Design, Synthesis, and Biological Evaluation of a Series of Acyclic Fleximer Nucleoside Antivirals. [D] . Peters, Hannah Louise. 2015

机译：一系列无环Fleximer核苷抗病毒药的设计，合成和生物学评估。
6. Synthesis and Biological Evaluation of a New Series of 124-triazolo15-a-135-triazines as Human A2A Adenosine Receptor Antagonists with Improved Water Solubility [O] . Stephanie Federico, Silvia Paoletta, Siew Lee Cheong, -1

机译：一种新的124-三唑的新系列的合成和生物学评价15-A -135-三嗪作为人A2A腺苷受体拮抗剂具有改善的水溶解度
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8. Targeting Adenosine A2A Receptors in Parkinson's Disease [R] . Schwarzschild, M. A. 2006

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Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.

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