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通过改进的高效方法制备的具有医学和农业潜在应用价值的抗真菌活性杂化(咪唑/苯并咪唑)-吡啶衍生物

Hybrid -(Imidazole/Benzimidazole)-Pyridine Derivatives with Antifungal Activity of Potential Interest in Medicine and Agriculture via Improved Efficiency Methods.

作者信息

Balaes Tiberius, Mangalagiu Violeta, Antoci Vasilichia, Amariucai-Mantu Dorina, Diaconu Dumitrela, Mangalagiu Ionel I

机构信息

Department of Biology, Faculty of Biology, Alexandru Ioan Cuza University of Iasi, 20A Carol 1st Bvd, 700505 Iasi, Romania.

Institute of Interdisciplinary Research, CERNESIM Centre, Alexandru Ioan Cuza University of Iasi, Bd. Carol I, No. 11, 700506 Iasi, Romania.

出版信息

Pharmaceuticals (Basel). 2025 Mar 28;18(4):495. doi: 10.3390/ph18040495.

DOI:10.3390/ph18040495
PMID:40283932
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12030448/
Abstract

: Nowadays fungal infections are rising serious threats for the human health system and agriculture, mostly because of antifungal resistance, emergence of new fungal pathogens and adverse effects, pressing the scientific world for exploration of new antifungal compounds. Therefore, the aim of this work was to synthesize and to study antifungal activity against human and plant fungi of a new class of hybrid -(imidazole/benzimidazole)-pyridine salt derivatives. : The synthesis of the hybrid derivatives was performed using both conventional thermal heating and ultrasound irradiation methods. : The use of ultrasound irradiation has the advantages of a dramatic decrease in reaction time and, consequently, a notable acceleration in reaction rate, a remarkable decrease in consumed energy and higher yields. The antifungal activity against five human fungal strains and for plant fungal strains was determined by the disk diffusion method and minimum inhibitory concentration. : The tested hybrid derivatives manifest good antifungal activity against the tested strains. Some of the hybrid compounds have very good quasi-nonselective activity against the tested human and plant pathogenic fungi, in some cases close to the control drug fluconazole, respectively, to many antifungal agents commercially used for plant protection.

摘要

如今,真菌感染对人类健康系统和农业构成了日益严重的威胁,主要原因是抗真菌耐药性、新真菌病原体的出现以及不良反应,这促使科学界探索新的抗真菌化合物。因此,本研究的目的是合成并研究一类新型杂化 -(咪唑/苯并咪唑)-吡啶盐衍生物对人和植物真菌的抗真菌活性。:杂化衍生物的合成采用了传统热加热和超声辐射两种方法。:超声辐射的使用具有反应时间显著缩短的优点,因此反应速率显著加快,能耗显著降低且产率更高。通过纸片扩散法和最低抑菌浓度测定了对五种人类真菌菌株和植物真菌菌株的抗真菌活性。:测试的杂化衍生物对测试菌株表现出良好的抗真菌活性。一些杂化化合物对测试的人和植物致病真菌具有非常好的准非选择性活性,在某些情况下分别接近对照药物氟康唑以及许多商业上用于植物保护的抗真菌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/b3110a143eef/pharmaceuticals-18-00495-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/74fbb65ffd22/pharmaceuticals-18-00495-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/6b074a237618/pharmaceuticals-18-00495-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/76b3f9379cf9/pharmaceuticals-18-00495-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/18e1f2a42667/pharmaceuticals-18-00495-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/b3110a143eef/pharmaceuticals-18-00495-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/74fbb65ffd22/pharmaceuticals-18-00495-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/6b074a237618/pharmaceuticals-18-00495-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/76b3f9379cf9/pharmaceuticals-18-00495-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/18e1f2a42667/pharmaceuticals-18-00495-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac92/12030448/b3110a143eef/pharmaceuticals-18-00495-sch002.jpg

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