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杂环化合物:基于合理结构考量的吡唑类似物药理学

Heterocyclic Compounds: Pharmacology of Pyrazole Analogs From Rational Structural Considerations.

作者信息

Costa Rafael Fernades, Turones Larissa Córdova, Cavalcante Keilah Valéria Naves, Rosa Júnior Ismael Aureliano, Xavier Carlos Henrique, Rosseto Lucimar Pinheiro, Napolitano Hamilton Barbosa, Castro Patrícia Ferreira da Silva, Neto Marcos Luiz Ferreira, Galvão Gustavo Mota, Menegatti Ricardo, Pedrino Gustavo Rodrigues, Costa Elson Alves, Martins José Luis Rodrigues, Fajemiroye James Oluwagbamigbe

机构信息

Universitary Center of Anápolis, UniEvangélica, Anápolis, Brazil.

Laboratory of Pharmacology of Natural and Synthetic Products, Institute of Biological Sciences, Federal University of Goiás, Goiânia, Brazil.

出版信息

Front Pharmacol. 2021 May 10;12:666725. doi: 10.3389/fphar.2021.666725. eCollection 2021.

Abstract

Low quality of life and life-threatening conditions often demand pharmacological screening of lead compounds. A spectrum of pharmacological activities has been attributed to pyrazole analogs. The substitution, replacement, or removal of functional groups on a pyrazole ring appears consistent with diverse molecular interactions, efficacy, and potency of these analogs. This mini-review explores cytotoxic, cytoprotective, antinociceptive, anti-inflammatory, and antidepressant activities of some pyrazole analogs to advance structure-related pharmacological profiles and rational design of new analogs. Numerous interactions of these derivatives at their targets could impact future research considerations and prospects while offering opportunities for optimizing therapeutic activity with fewer adverse effects.

摘要

生活质量低下和危及生命的状况常常需要对先导化合物进行药理学筛选。吡唑类似物具有一系列药理活性。吡唑环上官能团的取代、替换或去除似乎与这些类似物的多种分子相互作用、功效和效力相一致。这篇小型综述探讨了一些吡唑类似物的细胞毒性、细胞保护、抗伤害感受、抗炎和抗抑郁活性,以推进与结构相关的药理学概况以及新类似物的合理设计。这些衍生物在其靶点的众多相互作用可能会影响未来的研究考虑因素和前景,同时为优化治疗活性并减少不良反应提供机会。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f7cd/8141747/6134e66dca2b/fphar-12-666725-g001.jpg

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