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探讨查耳酮类和相关杂环化合物作为腺苷受体配体的应用:治疗学开发。

Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development.

机构信息

Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom, 2520, North West, South Africa.

Centre of Excellence for Pharmaceutical Sciences, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom, 2520, North West, South Africa.

出版信息

Mol Divers. 2022 Jun;26(3):1779-1821. doi: 10.1007/s11030-021-10257-9. Epub 2021 Jun 27.

Abstract

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.

摘要

腺苷受体 (ARs) 广泛分布于哺乳动物体内,参与了大量的生理和病理过程,而科学家们才刚刚开始破译这些过程。因此,AR 激动剂和拮抗剂一直是过去几十年来多个药物设计和开发项目的重点。在药物化学中,查尔酮结构被认为是一种特权支架,因此在这方面引起了相当大的兴趣。然而,由于其结构的潜在缺陷,有必要探索其他有潜力的化合物,如杂环化合物,过去已经成功地从查尔酮前体中获得了这些化合物。这篇综述旨在总结腺苷受体及其配体的新兴治疗重要性,特别是在中枢神经系统 (CNS) 中,同时强调查尔酮和杂环衍生物作为有前途的 AR 配体先导化合物。

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