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基于1,3,4-噻二唑的化合物的生物学和药理学活性。

Biological and pharmacological activities of 1,3,4-thiadiazole based compounds.

作者信息

Matysiak Joanna

机构信息

Department of Chemistry, University of Life Sciences in Lublin, Akademicka 15, 20-950 Lublin, Poland.

出版信息

Mini Rev Med Chem. 2015;15(9):762-75. doi: 10.2174/1389557515666150519104057.

Abstract

The chemistry of 1,3,4-thiadiazoles is very well known. A universal and commonly used method of the synthesis of different 2,5-disubstituted 1,3,4-thiadiazoles includes the cyclization of appropriate linear organic derivatives. They are widely known as compounds with various kinds of biological activities showing anticancer properties against human cancers and acting as diuretic, antibacterial, antifungal, antitubercular and leishmanicidal agents. Many of them influence on OUN exhibiting anticonvulsant, anti-inflammatory, antidepressant, analgesic and anxiolytic effects. The molecular target of 1,3,4-thiadiazoles includes the following enzymes: carbonic anhydrase (CA), cyclooxygenase (CO), neutral endopeptidase (NEP), aminopeptidase N (APN), matrix metalloproteinases (MMPs), phosphodiesterases (PDEs) and c-Src/Abl tyrosine kinase. In this presentation, recent achievements in the medicinal chemistry of 1,3,4-thiadiazole based compounds are reviewed.

摘要

1,3,4-噻二唑的化学性质广为人知。一种通用且常用的合成不同2,5-二取代1,3,4-噻二唑的方法包括合适的线性有机衍生物的环化反应。它们作为具有各种生物活性的化合物而广为人知,这些生物活性包括对人类癌症具有抗癌特性,以及作为利尿剂、抗菌剂、抗真菌剂、抗结核剂和抗利什曼原虫剂。其中许多还对神经系统产生影响,表现出抗惊厥、抗炎、抗抑郁、镇痛和抗焦虑作用。1,3,4-噻二唑的分子靶点包括以下几种酶:碳酸酐酶(CA)、环氧化酶(CO)、中性内肽酶(NEP)、氨肽酶N(APN)、基质金属蛋白酶(MMPs)、磷酸二酯酶(PDEs)和c-Src/Abl酪氨酸激酶。在本报告中,对基于1,3,4-噻二唑的化合物的药物化学最新进展进行了综述。

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