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噻唑烷类:抗禽流感和传染性支气管炎病毒的潜在抗病毒剂。

Thiazolidines: Potential anti-viral agents against avian influenza and infectious bronchitis viruses.

作者信息

Musaddiq Sara, Imran Shahzad Mirza, Firdous Farzana, Iqbal Atia, Tanveer Mehwish, Ashraf Abida, Aslam Samina, Khakwani Samia

机构信息

Department of Chemistry, Faculty of Science, The Women University Multan, Multan, Pakistan.

Department of Biochemistry, Faculty of Science, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.

出版信息

Vet Res Forum. 2020 Fall;11(4):415-421. doi: 10.30466/vrf.2018.91264.2211. Epub 2020 Dec 15.

Abstract

Viral outbreaks are a common cause of morbidity and mortality in livestock and human populations. Lack of good vaccines and poor control measures along with natural viral genetic drifting and shifting are the common causes of new viral strains and outbreaks. The current study reports the synthesis of some 2-aryl substituted thiazolidine-4-carboxylic acids 1a-h and their 3-acetyl 2a and 3-benzoyl derivatives 3a. Two important poultry viruses: Avian influenza virus (AIV; A/Chicken/Italy/1994/H9N2) and infectious bronchitis virus (IBV) were selected, grown in ‎9-11 days old chicken embryonated eggs‎, and subjected to anti-viral assays. Most of the synthesized compounds were found active against AIV subtype H9N2 and IBV. In the case of AIV, the best results were attained for compound 1d which showed an IC value of 3.47 µM, while IBV 1c showed IC value of 4.10 µM. The lower IC values of these compounds correlate with the high potency of these compounds, especially in comparison with control groups. The standard drugs amantadine and ribavarin were used as positive controls in the case of AIV and IBV, respectively. Better results were obtained with 2-aryl substituted thiazolidine-4-carboxylic acids 1a-h compared to their -acylated derivatives 2a and 3a against both viruses. In conclusion, this preliminary data support the idea that thiazolidine carboxylic acids could be used as anti-viral drugs against AIV and IBV infections.

摘要

病毒爆发是家畜和人类发病和死亡的常见原因。缺乏优质疫苗、控制措施不力,以及病毒自然的基因漂移和变异,是新病毒株出现和爆发的常见原因。本研究报告了一些2-芳基取代的噻唑烷-4-羧酸1a-h及其3-乙酰基衍生物2a和3-苯甲酰基衍生物3a的合成。选择了两种重要的家禽病毒:禽流感病毒(AIV;A/Chicken/Italy/1994/H9N2)和传染性支气管炎病毒(IBV),在9-11日龄鸡胚中培养,并进行抗病毒试验。发现大多数合成化合物对AIV H9N2亚型和IBV具有活性。对于AIV,化合物1d表现最佳,IC值为3.47µM,而对于IBV,化合物1c的IC值为4.10µM。这些化合物较低的IC值与其高效能相关,尤其是与对照组相比。在AIV和IBV试验中,分别使用标准药物金刚烷胺和利巴韦林作为阳性对照。与它们的酰化衍生物2a和3a相比,2-芳基取代的噻唑烷-4-羧酸1a-h对两种病毒均取得了更好的结果。总之,这些初步数据支持噻唑烷羧酸可作为抗AIV和IBV感染的抗病毒药物这一观点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6153/7904115/f8721e80ce0e/vrf-11-415-g001.jpg

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