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肉桂醛的基于唑类的乙酰肼衍生物通过诱导细胞凋亡来靶向并杀死(细胞)。

Azole Based Acetohydrazide Derivatives of Cinnamaldehyde Target and Kill by Causing Cellular Apoptosis.

作者信息

Wani Mohmmad Younus, Ahmad Aijaz, Aqlan Faisal Mohammed, Al-Bogami Abdullah Saad

机构信息

University of Jeddah, College of Science, Department of Chemistry, Jeddah 21589, Saudi Arabia.

Clinical Microbiology and Infectious Diseases, School of Pathology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg 2193, South Africa.

出版信息

ACS Med Chem Lett. 2020 Feb 5;11(4):566-574. doi: 10.1021/acsmedchemlett.0c00030. eCollection 2020 Apr 9.

Abstract

Opportunistic fungal pathogens including are responsible for the alarming rise in hospital acquired infections and millions of deaths worldwide. The current treatment modalities are not enough to handle this situation, and therefore, new treatment modalities and strategies are desperately needed. In this direction, we synthesized a series of azole based acetohydrazide derivatives of cinnamaldehyde and subjected it to antifungal activity evaluation. Preliminary antifungal activity evaluation revealed tremendous antifungal potential of some of the derivatives against fluconazole susceptible and resistant clinical isolates of . Although all the compounds in the series are structurally similar except for the presence of different substituents on the phenyl ring of the acetohydrazide pendent, they sharply differed in their activity profile. Further mechanism of action studies revealed that these compounds have an apoptotic effect on confirmed via Annexin V-FITC staining and TUNEL assay.

摘要

包括[具体真菌病原体未给出]在内的机会性真菌病原体是导致医院获得性感染惊人增加以及全球数百万人死亡的原因。当前的治疗方式不足以应对这种情况,因此,迫切需要新的治疗方式和策略。在这个方向上,我们合成了一系列肉桂醛的基于唑的乙酰肼衍生物,并对其进行抗真菌活性评估。初步抗真菌活性评估显示,一些衍生物对氟康唑敏感和耐药的[具体真菌未给出]临床分离株具有巨大的抗真菌潜力。尽管该系列中的所有化合物在结构上相似,只是乙酰肼侧链苯环上存在不同取代基,但它们的活性谱却有很大差异。进一步的作用机制研究表明,这些化合物对[具体真菌未给出]具有凋亡作用,这通过膜联蛋白V - FITC染色和TUNEL检测得以证实。

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Antifungal resistance: current trends and future strategies to combat.抗真菌耐药性:当前趋势及应对的未来策略
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