1,3,4-噻二唑衍生物的抗菌活性。

IF 4.8 3区 医学 Q2 CHEMISTRY, MEDICINAL
Pharmaceuticals Pub Date : 2025-09-08 DOI:10.3390/ph18091348
Sebastian Górecki, Agnieszka Kudelko, Monika Olesiejuk
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引用次数: 0

摘要

1,3,4-噻二唑核由于其独特的电子结构、物理化学性质和广泛的药理潜力而引起了广泛的关注。这种杂环支架具有广泛的生物活性,通常归因于其调节酶功能的能力,与受体相互作用,并破坏病原体和宿主细胞中的关键生化途径。此外,1,3,4-噻二唑通常具有良好的药代动力学特性,包括高代谢稳定性和适当的亲脂性,这增强了它们的药物相似性和生物利用度。本文综述了近五年来报道的含有1,3,4-噻二唑支架的抗菌和抗真菌化合物。该出版物详细介绍了新型1,3,4-噻二唑衍生物的化学结构,并报告了针对一系列微生物菌株进行的抗菌和抗真菌活性测定的结果。此外,它还提供了有关影响所合成化合物的观察到的生物活性的结构特征的结论。对10株革兰氏阴性菌和9株革兰氏阳性菌的抑菌活性评估表明,79种新合成的1,3,4-噻二唑衍生物要么表现出优于标准参考抗生素的抑菌效果,要么实现了高水平的细菌生长抑制,定义为90-100%的抑制。在抗真菌试验中,化合物对代表15属的25种真菌进行了评价。在测试的衍生物中,75个化合物的抗真菌效力超过了参考抗真菌剂,或者在90-100%的范围内产生了生长抑制。本文提供的信息可作为从事开发新型候选药物和植物保护剂的医药和农业化学家的宝贵资源。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Antimicrobial Activity of 1,3,4-Thiadiazole Derivatives.

The 1,3,4-thiadiazole core has attracted significant attention due to its unique electronic structure, physicochemical properties, and wide-ranging pharmacological potential. This heterocyclic scaffold exhibits a broad spectrum of biological activities, often attributed to its capacity to modulate enzyme function, interact with receptors, and disrupt key biochemical pathways in both pathogens and host cells. Additionally, 1,3,4-thiadiazoles typically display favorable pharmacokinetic properties, including high metabolic stability and appropriate lipophilicity, which enhance their drug-likeness and bioavailability. This review presents an overview of antibacterial and antifungal compounds bearing the 1,3,4-thiadiazole scaffold that have been reported over the past five years. This publication details the chemical structures of novel 1,3,4-thiadiazole derivatives and reports the results of antibacterial and antifungal activity assays conducted against a range of microbial strains. Furthermore, it provides conclusions regarding the structural features that influence the observed biological activity of the synthesized compounds. Antimicrobial activity assessments conducted against ten Gram-negative and nine Gram-positive bacterial strains revealed that 79 newly synthesized 1,3,4-thiadiazole derivatives exhibited either superior inhibitory efficacy relative to standard reference antibiotics or achieved a high level of bacterial growth suppression, defined as 90-100% inhibition. In antifungal assays, the compounds were evaluated against 25 fungal species representing 15 genera. Among the tested derivatives, 75 compounds demonstrated antifungal potency exceeding that of reference antifungal agents or produced growth inhibition within the 90-100% range. The information provided herein may serve as a valuable resource for medicinal and agricultural chemists engaged in the development of novel drug candidates and plant protection agents.

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来源期刊
Pharmaceuticals
Pharmaceuticals Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.10
自引率
4.30%
发文量
1332
审稿时长
6 weeks
期刊介绍: Pharmaceuticals (ISSN 1424-8247) is an international scientific journal of medicinal chemistry and related drug sciences.Our aim is to publish updated reviews as well as research articles with comprehensive theoretical and experimental details. Short communications are also accepted; therefore, there is no restriction on the maximum length of the papers.
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