학술논문
Synthesis and evaluation of two series of 4′-aza-carbocyclic nucleosides as adenosine A2A receptor agonists
Document Type
Article
Author
Source
Subject
*ORGANIC synthesis
*NUCLEOSIDES
*HETEROCYCLIC compounds
*SUBSTITUTION reactions
*DRUG synergism
*ANTI-inflammatory agents
*AMIDES
*THERAPEUTICS
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Language
ISSN
0960-894X
Abstract
Abstract: 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 A2A 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. [Copyright &y& Elsevier]