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三唑类化合物的合成方法及抗真菌活性研究进展。

Advances in synthetic approach to and antifungal activity of triazoles.

机构信息

Department of Pharmaceutical Technology, Meerut Institute of Engineering & Technology, Meerut, U. P., India, Pin-250005.

出版信息

Beilstein J Org Chem. 2011;7:668-77. doi: 10.3762/bjoc.7.79. Epub 2011 May 25.

Abstract

Several five membered ring systems, e.g., triazole, oxadiazole dithiazole and thiadiazole with three heteroatoms at symmetrical or asymmetrical positions have been studied because of their interesting pharmacological properties. In this article our emphasis is on synthetic development and pharmacological activity of the triazole moiety which exhibit a broad spectrum of pharmacological activity such as antifungal, antibacterial, anti-inflammatory and anticancer etc. Triazoles have increased our ability to treat many fungal infections, for example, candidiasis, cryptococcal meningitis, aspergillosis etc. However, mortality due to these infections even with antifungal therapy is still unacceptably high. Therefore, the development of new antifungal agents targeting specific fungal structures or functions is being actively pursued. Rapid developments in molecular mycology have led to a concentrated search for more target antifungals. Although we are entering a new era of antifungal therapy in which we will continue to be challenged by systemic fungal diseases, the options for treatment will have greatly expanded.

摘要

一些五元环系统,例如三唑、恶二唑、二硫代恶唑和噻二唑,由于其具有有趣的药理学性质,因此在对称或不对称位置上具有三个杂原子。本文重点介绍了三唑部分的合成发展和药理学活性,该部分具有广泛的药理学活性,如抗真菌、抗菌、抗炎和抗癌等。三唑类化合物提高了我们治疗许多真菌感染的能力,例如念珠菌病、隐球菌性脑膜炎、曲霉菌病等。然而,即使进行抗真菌治疗,这些感染的死亡率仍然高得令人无法接受。因此,正在积极开发针对特定真菌结构或功能的新型抗真菌药物。分子真菌学的快速发展导致了对更多靶向抗真菌药物的集中研究。尽管我们正在进入一个新的抗真菌治疗时代,我们将继续受到系统性真菌感染的挑战,但治疗选择将大大扩大。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a29b/3135122/a6379ffc8af6/Beilstein_J_Org_Chem-07-668-g002.jpg

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