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带有侧链吲哚环的新型过渡金属配合物：对其抗真菌活性及作用方式的深入研究

New transition metal complexes with a pendent indole ring: insights into the antifungal activity and mode of action.

作者信息

Dar Ovas Ahmad, Lone Shabir Ahmad, Malik Manzoor Ahmad, Wani Mohmmad Younus, Ahmad Aijaz, Hashmi Athar Adil

机构信息

Department of Chemistry, Jamia Millia Islamia New Delhi 110025 India

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

出版信息

RSC Adv. 2019 May 14;9(27):15151-15157. doi: 10.1039/c9ra02600b.

DOI:10.1039/c9ra02600b
PMID:35514852
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9064211/
Abstract

Development of new chemotherapeutic agents to treat multidrug-resistant fungal infections to augment the current treatment options is a must. In this direction, a series of mixed ligand complexes was synthesized from a Schiff base (L) obtained by the condensation of 2-hydroxynapthaldehyde and tryptamine, and 1,10-phenanthroline (1,10-phen) as a secondary ligand. Based on spectral characterization and physical measurements an octahedral geometry was assigned to [Co(phen)LClHO] (C2), Ni(phen)LClHO, and Zn(phen)LClHO complexes while a distorted octahedral geometry was assigned to the Cu(phen)LClHO complex. All the synthesized compounds were tested for antifungal activity against 11 isolates, including fluconazole (FLC) resistant isolates, by determining minimum inhibitory concentrations and studying growth curves. MIC results suggest that all the newly synthesized compounds have potent antifungal activity at varying levels. The rapid action of these compounds on fungal cells suggested a membrane-located target for their action.

摘要

开发新的化疗药物以治疗多重耐药真菌感染，从而增加当前的治疗选择是必不可少的。在这个方向上，一系列混合配体配合物由2-羟基萘甲醛与色胺缩合得到的席夫碱（L）和作为第二配体的1,10-菲咯啉（1,10-phen）合成。基于光谱表征和物理测量，[Co(phen)LClHO]（C2）、Ni(phen)LClHO和Zn(phen)LClHO配合物被指定为八面体几何构型，而Cu(phen)LClHO配合物被指定为扭曲的八面体几何构型。通过测定最低抑菌浓度并研究生长曲线，对所有合成化合物针对11种分离株（包括耐氟康唑（FLC）分离株）进行了抗真菌活性测试。MIC结果表明，所有新合成的化合物都具有不同程度的强效抗真菌活性。这些化合物对真菌细胞的快速作用表明其作用靶点位于细胞膜上。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/5b98c33f3181/c9ra02600b-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/9cba7483d1b8/c9ra02600b-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/4c3033bbe71b/c9ra02600b-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/9eb5f4eb6ed2/c9ra02600b-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/5b98c33f3181/c9ra02600b-f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/9cba7483d1b8/c9ra02600b-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/4c3033bbe71b/c9ra02600b-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/9eb5f4eb6ed2/c9ra02600b-f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1d52/9064211/5b98c33f3181/c9ra02600b-f3.jpg

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