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噻二唑的合成方法、化学性质及抗惊厥活性

Synthetic methods, chemistry, and the anticonvulsant activity of thiadiazoles.

作者信息

Sharma Bhawna, Verma Amita, Prajapati Sunil, Sharma Upendra Kumar

机构信息

Institute of Pharmacy, Bundelkhand University, Jhansi 284128, India.

Department of Pharmaceutical Sciences, Faculty of Health Sciences, Sam Higginbottom Institute of Agriculture, Technology and Sciences-Deemed University, Allahabad 211007, India.

出版信息

Int J Med Chem. 2013;2013:348948. doi: 10.1155/2013/348948. Epub 2013 Apr 30.

DOI:10.1155/2013/348948
PMID:25405032
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4207456/
Abstract

The chemistry of heterocyclic compounds has been an interesting field of study for a long time. Heterocyclic nucleus 1,3,4-thiadiazole constitutes an important class of compounds for new drug development. The synthesis of novel thiadiazole derivatives and investigation of their chemical and biological behavior have gained more importance in recent decades. The search for antiepileptic compounds with more selective activity and lower toxicity continues to be an active area of intensive investigation in medicinal chemistry. During the recent years, there has been intense investigation of different classes of thiadiazole compounds, many of which possess extensive pharmacological activities, namely, antimicrobial activity, anticonvulsant, antifungal antidiabetic, anti-inflammatory, antioxidant, and antituberculosis activities, and so forth. The resistance towards available drugs is rapidly becoming a major worldwide problem. The need to design new compounds to deal with this resistance has become one of the most important areas of research today. Thiadiazole is a versatile moiety that exhibits a wide variety of biological activities. Thiadiazole moiety acts as "hydrogen binding domain" and "two-electron donor system." It also acts as a constrained pharmacophore. On the basis of the reported literature, we study here thiadiazole compounds and their synthetic methods chemistry and anticonvulsant activity.

摘要

长期以来,杂环化合物的化学一直是一个有趣的研究领域。杂环核1,3,4-噻二唑构成了新药开发中一类重要的化合物。近几十年来,新型噻二唑衍生物的合成及其化学和生物学行为的研究变得更加重要。寻找具有更高选择性活性和更低毒性的抗癫痫化合物仍然是药物化学中一个积极深入研究的领域。近年来,人们对不同类别的噻二唑化合物进行了深入研究,其中许多具有广泛的药理活性,即抗菌活性、抗惊厥、抗真菌、抗糖尿病、抗炎、抗氧化和抗结核活性等等。对现有药物的耐药性正迅速成为一个全球性的主要问题。设计新化合物以应对这种耐药性的需求已成为当今最重要的研究领域之一。噻二唑是一个具有多种生物活性的通用部分。噻二唑部分充当“氢键结合域”和“双电子供体系统”。它还充当一个受限的药效团。基于已报道的文献,我们在此研究噻二唑化合物及其合成方法、化学性质和抗惊厥活性。

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