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1,3,4-噻二唑类似物作为潜在骨架的合成及其抗菌活性评价

Synthesis and Evaluation of Antimicrobial Activity of 1, 3, 4-Thiadiazole Analogues for Potential Scaffold.

作者信息

Sahu Sagar, Sahu Tanesh, Kalyani Gunjan, Gidwani Bina

机构信息

Columbia Institute of Pharmacy, Raipur, India.

Shri Rawatpura Sarkar Institute of Pharmacy, Kumhari, India.

出版信息

J Pharmacopuncture. 2021 Mar 31;24(1):32-40. doi: 10.3831/KPI.2021.24.1.32.

DOI:10.3831/KPI.2021.24.1.32
PMID:33833898
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8010424/
Abstract

OBJECTIVES

Pathogenic microbes are causal agents for various types of severe and even lethal infectious diseases. Despite of development in medication, bacterial and fungal infections still persist to be a vital problem in health care. Bacteria and several fungal species have shown resistance to antibiotics used in treatment to current medications. Therefore, it is a considerable field of interest in the design and development of novel compounds with antimicrobial activity.

METHODS

The compounds bearing a heterocyclic ring play an imperative role among other organic compounds with pharmacological activity used as drugs in human for control and cure of various infections. Thiadiazoles containing nitrogen-sulfur atom as part of their cyclic structure which shown wide-ranging application as structural units of biologically active molecules and are very useful intermediates in Medicinal Chemistry.

RESULTS

The effectiveness of the thiadiazole nucleus was established by the drugs currently used for the treatment of various infections. 1,3,4-Thiadiazoles and some of their derivatives are widely studied because of their broad spectrum of pharmacological activities.

CONCLUSION

In the present work, a series of 1,3,4-Thiadiazole derivatives were synthesized by cyclization of a group of various benzaldehyde with thiosemicarbazide in the presence of various reagent like FeCl, HCHO by losing a molecule of water. These derivatives were found to possess prominent antimicrobial activity.

摘要

目标

致病微生物是各类严重甚至致命传染病的病原体。尽管药物有所发展,但细菌和真菌感染仍是医疗保健中的一个重要问题。细菌和几种真菌已对目前治疗用药中使用的抗生素产生耐药性。因此,新型抗菌活性化合物的设计与开发是一个备受关注的领域。

方法

带有杂环的化合物在用作人类控制和治疗各种感染药物的具有药理活性的其他有机化合物中起着至关重要的作用。含有氮硫原子作为其环状结构一部分的噻二唑,作为生物活性分子的结构单元显示出广泛的应用,并且是药物化学中非常有用的中间体。

结果

目前用于治疗各种感染的药物证实了噻二唑核的有效性。1,3,4 - 噻二唑及其一些衍生物因其广泛的药理活性而被广泛研究。

结论

在本研究中,通过一组各种苯甲醛与氨基硫脲在诸如氯化铁、甲醛等各种试剂存在下环化并失去一分子水,合成了一系列1,3,4 - 噻二唑衍生物。发现这些衍生物具有显著的抗菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/35c81398bc4f/JoP-24-1-32-f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/93854d795b11/JoP-24-1-32-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/a84287b3e251/JoP-24-1-32-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/15de7b0ee519/JoP-24-1-32-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/062757c63326/JoP-24-1-32-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/7d3d31efd48a/JoP-24-1-32-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/906e9a875ffb/JoP-24-1-32-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/e28cb4b62b57/JoP-24-1-32-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/915a7c81f7c1/JoP-24-1-32-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/35c81398bc4f/JoP-24-1-32-f9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/93854d795b11/JoP-24-1-32-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/a84287b3e251/JoP-24-1-32-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/15de7b0ee519/JoP-24-1-32-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/062757c63326/JoP-24-1-32-f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/7d3d31efd48a/JoP-24-1-32-f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/906e9a875ffb/JoP-24-1-32-f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/e28cb4b62b57/JoP-24-1-32-f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/915a7c81f7c1/JoP-24-1-32-f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9208/8010424/35c81398bc4f/JoP-24-1-32-f9.jpg

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1,3,4-thiadiazole and its derivatives: a review on recent progress in biological activities.1,3,4-噻二唑及其衍生物:生物活性的最新研究进展综述。
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