Molecular Diversity ( IF 3.9 ) Pub Date : 2021-06-27 , DOI: 10.1007/s11030-021-10257-9 Chrisna Matthee 1 , Gisella Terre'Blanche 1, 2 , Lesetja J Legoabe 2 , Helena D Janse van Rensburg 1
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Adenosine receptors (ARs) are ubiquitously distributed throughout the mammalian body where they are involved in an extensive list of physiological and pathological processes that scientists have only begun to decipher. Resultantly, AR agonists and antagonists have been the focus of multiple drug design and development programmes within the past few decades. Considered to be a privileged scaffold in medicinal chemistry, the chalcone framework has attracted a substantial amount of interest in this regard. Due to the potential liabilities associated with its structure, however, it has become necessary to explore other potentially promising compounds, such as heterocycles, which have successfully been obtained from chalcone precursors in the past. This review aims to summarise the emerging therapeutic importance of adenosine receptors and their ligands, especially in the central nervous system (CNS), while highlighting chalcone and heterocyclic derivatives as promising AR ligand lead compounds.
Graphic abstract
中文翻译：
查耳酮及相关杂环化合物作为腺苷受体配体的探索：治疗发展
腺苷受体 (ARs) 普遍分布在整个哺乳动物体内，它们参与了科学家刚刚开始破译的大量生理和病理过程。因此，在过去的几十年里，AR 激动剂和拮抗剂一直是多个药物设计和开发项目的重点。查耳酮框架被认为是药物化学中的一种特殊支架，在这方面引起了极大的兴趣。然而，由于与其结构相关的潜在责任，有必要探索其他有潜力的化合物，例如杂环化合物，这些化合物过去已成功地从查尔酮前体中获得。
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