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苯并三唑：关于其多样生物学行为的概述

Benzotriazole: An overview on its versatile biological behavior.

作者信息

Briguglio I, Piras S, Corona P, Gavini E, Nieddu M, Boatto G, Carta A

机构信息

Department of Chemistry and Pharmacy, University of Sassari, Via Muroni 23/A, 07100 Sassari, Italy.

Department of Chemistry and Pharmacy, University of Sassari, Via Muroni 23/A, 07100 Sassari, Italy.

出版信息

Eur J Med Chem. 2015 Jun 5;97:612-48. doi: 10.1016/j.ejmech.2014.09.089. Epub 2014 Sep 30.

DOI:10.1016/j.ejmech.2014.09.089
PMID:25293580
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7115563/
Abstract

Discovered in late 1960, azoles are heterocyclic compounds class which constitute the largest group of available antifungal drugs. Particularly, the imidazole ring is the chemical component that confers activity to azoles. Triazoles are obtained by a slight modification of this ring and similar or improved activities as well as less adverse effects are reported for triazole derivatives. Consequently, it is not surprising that benzimidazole/benzotriazole derivatives have been found to be biologically active. Since benzimidazole has been widely investigated, this review is focused on defining the place of benzotriazole derivatives in biomedical research, highlighting their versatile biological properties, the mode of action and Structure Activity Relationship (SAR) studies for a variety of antimicrobial, antiparasitic, and even antitumor, choleretic, cholesterol-lowering agents.

摘要

唑类于1960年末被发现，是杂环化合物类别，构成了现有抗真菌药物中最大的一组。特别是，咪唑环是赋予唑类活性的化学成分。三唑类是通过对该环进行轻微修饰而获得的，据报道三唑衍生物具有相似或更好的活性以及更少的不良反应。因此，发现苯并咪唑/苯并三唑衍生物具有生物活性也就不足为奇了。由于苯并咪唑已得到广泛研究，本综述重点在于确定苯并三唑衍生物在生物医学研究中的地位，突出其多样的生物学特性、作用方式以及针对多种抗菌、抗寄生虫乃至抗肿瘤、利胆、降胆固醇药物的构效关系（SAR）研究。

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Mycopathologia. 2013 Apr;175(3-4):345-9. doi: 10.1007/s11046-012-9610-3. Epub 2013 Jan 20.
9
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists.合成及氨基噻唑并苯并氮杂卓的 SAR 研究作为选择性多巴胺 D2 部分激动剂。
Bioorg Med Chem Lett. 2013 Jan 15;23(2):543-7. doi: 10.1016/j.bmcl.2012.11.023. Epub 2012 Nov 28.
10
Benzimidazole derivatives as potential anticancer agents.苯并咪唑衍生物作为潜在的抗癌剂。
Mini Rev Med Chem. 2013 Mar;13(3):399-407. doi: 10.2174/138955713804999847.