Novel thiazolidine-4-carboxylic acid derivatives: synthesis and inhibitory effects against influenza A.

IF 3.4 4区医学 Q3 CHEMISTRY, MEDICINAL

Future medicinal chemistry Pub Date : 2025-10-01 Epub Date: 2025-09-12 DOI:10.1080/17568919.2025.2559575

Muazzam Arif, Humaira Nadeem, Zaman Ashraf, Muhammad Tariq Khan, Tayyaba Anwar, Rizwan Hafeez

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引用次数: 0

Abstract

Aims: This study explored the synthesis and evaluation of novel neuraminidase (NA) inhibitors, focusing on thiazolidine-4-carboxylic acid derivatives to combat influenza.

Materials and methods: The synthesized compounds were evaluated for their NA inhibitory activity and assessed against Influenza A (H7N3) using hemagglutination inhibition (HAI) assays. Molecular docking studies were also conducted to support the experimental findings.

Results: Compounds 4a, 4b, and 6a demonstrated potent NA inhibitory activity. While all compounds showed moderate HAI activity compared to Oseltamivir, 4a and 8a exhibited strong potency with low Mean MIC values against the H7N3 strain.

Conclusions: These findings suggest that the thiazolidine derivatives hold potential as novel inhibitory agents against influenza. Future research will focus on assessing their toxicity and safety profiles, paving the way for the development of effective and safer NA inhibitors.

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新型噻唑烷-4-羧酸衍生物的合成及其对甲型流感的抑制作用。

目的：探讨新型神经氨酸酶（NA）抑制剂的合成与评价，重点研究噻唑烷-4-羧酸衍生物抗流感的作用。材料与方法：采用血凝抑制（HAI）法测定合成的化合物对甲型h1n1流感病毒（H7N3）的抑制活性。分子对接研究也支持了实验结果。结果：化合物4a、4b和6a具有较强的NA抑制活性。与奥司他韦相比，所有化合物均表现出中等的抗HAI活性，但4a和8a对H7N3病毒表现出较强的效力，平均MIC值较低。结论：这些发现表明噻唑烷衍生物具有作为新型流感抑制剂的潜力。未来的研究将集中于评估它们的毒性和安全性，为开发更有效和更安全的NA抑制剂铺平道路。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Future medicinal chemistry CHEMISTRY, MEDICINAL-

CiteScore

5.80

自引率

2.40%

发文量

118

审稿时长

4-8 weeks

期刊介绍： Future Medicinal Chemistry offers a forum for the rapid publication of original research and critical reviews of the latest milestones in the field. Strong emphasis is placed on ensuring that the journal stimulates awareness of issues that are anticipated to play an increasingly central role in influencing the future direction of pharmaceutical chemistry. Where relevant, contributions are also actively encouraged on areas as diverse as biotechnology, enzymology, green chemistry, genomics, immunology, materials science, neglected diseases and orphan drugs, pharmacogenomics, proteomics and toxicology.