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含氮杂环类药物化学化合物的生物评价概述。

An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds.

机构信息

Department of Chemistry, Faculty of Natural Science, Mangosuthu University of Technology, Umlazi 4031, KZN, South Africa.

Department of Physics, University of Alberta, Edmonton, AB T6G 2E1, Canada.

出版信息

Int J Mol Sci. 2022 Jul 23;23(15):8117. doi: 10.3390/ijms23158117.

DOI:10.3390/ijms23158117
PMID:35897691
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9368212/
Abstract

Heterocyclic compounds are a class of compounds of natural origin with favorable properties and hence have major pharmaceutical significance. They have an exceptional adroitness favoring their use as diverse smart biomimetics, in addition to possessing an active pharmacophore in a complex structure. This has made them an indispensable motif in the drug discovery field. Heterocyclic compounds are usually classified according to the ring size, type, and the number of heteroatoms present in the ring. Among different heterocyclic ring systems, nitrogen heterocyclic compounds are more abundant in nature. They also have considerable pharmacological significance. This review highlights recent pioneering studies in the biological assessment of nitrogen-containing compounds, namely: triazoles, tetrazoles, imidazole/benzimidazoles, pyrimidines, and quinolines. It explores publications between April 2020 and February 2022 and will benefit researchers in medicinal chemistry and pharmacology. The present work is organized based on the size of the heterocyclic ring.

摘要

杂环化合物是一类具有优良性质的天然来源化合物,因此具有重要的药物意义。它们具有特殊的灵巧性,除了在复杂结构中具有活性药效团外,还可以作为多种智能仿生药物使用。这使它们成为药物发现领域不可或缺的主题。杂环化合物通常根据环的大小、类型和环中存在的杂原子的数量进行分类。在不同的杂环环系中,含氮杂环化合物在自然界中更为丰富。它们也具有相当大的药理学意义。本综述重点介绍了含氮化合物的生物学评估的最新开创性研究,即:三唑、四唑、咪唑/苯并咪唑、嘧啶和喹啉。它探讨了 2020 年 4 月至 2022 年 2 月之间的出版物,将使药物化学和药理学领域的研究人员受益。本工作根据杂环的大小进行组织。

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Bioorg Chem. 2022 Feb;119:105485. doi: 10.1016/j.bioorg.2021.105485. Epub 2021 Nov 20.
8
Design, Synthesis, and Antiviral activity of 1,2,3,4-Tetrahydropyrimidine derivatives acting as novel entry inhibitors to target at "Phe43 cavity" of HIV-1 gp120.设计、合成及抗病毒活性的 1,2,3,4-四氢嘧啶衍生物作为新型进入抑制剂作用靶点的"phe43 腔"的 HIV-1 gp120。
Bioorg Med Chem. 2021 Dec 15;52:116526. doi: 10.1016/j.bmc.2021.116526. Epub 2021 Nov 20.
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Design, synthesis and biological evaluation of 1,5-disubstituted α-amino tetrazole derivatives as non-covalent inflammasome-caspase-1 complex inhibitors with potential application against immune and inflammatory disorders.设计、合成及生物评价 1,5-取代-α-氨基四唑衍生物作为非共价型炎症小体-caspase-1 复合物抑制剂用于治疗免疫和炎症性疾病的应用潜力。
Eur J Med Chem. 2022 Feb 5;229:114002. doi: 10.1016/j.ejmech.2021.114002. Epub 2021 Nov 18.
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Design, synthesis and biological evaluation of 7-((7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)-2,3-dihydro-1H-inden-1-one derivatives as potent FAK inhibitors for the treatment of ovarian cancer.设计、合成及生物评价 7-((7H-吡咯并[2,3-d]嘧啶-4-基)氧基)-2,3-二氢-1H-茚-1-酮衍生物作为潜在的卵巢癌治疗用 FAK 抑制剂。
Eur J Med Chem. 2022 Jan 15;228:113978. doi: 10.1016/j.ejmech.2021.113978. Epub 2021 Nov 11.