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Adenosine A2A receptor antagonists as novel anti-Parkinsonian agents: a review of structure-activity relationships.

机译:腺苷A2A受体拮抗剂作为新型抗帕金森病药物:结构-活性关系的综述。

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摘要

The adenosine A2A receptor (AA2AR) has emerged as an attractive target for the treatment of Parkinson's disease. Evidence suggests that antagonists of the AA2AR may be neuroprotective and may help to alleviate the symptoms of Parkinson's disease. During last decade, many efforts have been accomplished searching potent and selective AA2AR antagonists. In this field, various xanthines and non-xanthine heterocyclic compounds of monocyclic, bicyclic and tricyclic nucleus possessing very good affinity with a broad range of selectivity have been proposed. The aim of this article is to summarize available data on different chemical classes of AA2AR antagonists including those in clinical development, and briefly present an overview of the structure-activity relationships found for these compounds.
机译:腺苷A2A受体(AA2AR)已成为治疗帕金森氏病的诱人靶标。有证据表明,AA2AR的拮抗剂可能具有神经保护作用,可能有助于减轻帕金森氏病的症状。在过去的十年中,已经完成了许多寻找有效和选择性AA2AR拮抗剂的努力。在该领域中,已经提出了具有非常好的亲和性和广泛的选择性的各种单环,双环和三环核的黄嘌呤和非黄嘌呤杂环化合物。本文的目的是总结有关AA2AR拮抗剂不同化学类别的可用数据,包括临床开发中的那些,并简要介绍这些化合物的构效关系。

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