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对喹唑啉-4(3)-酮衍生席夫碱及其铜(II)配合物的抗菌、抗生物膜和细胞毒性活性的批判性观点。

Critical view on antimicrobial, antibiofilm and cytotoxic activities of quinazolin-4(3)-one derived schiff bases and their Cu(II) complexes.

作者信息

Pindjakova Dominika, Mascaretti Sarka, Hricoviniova Jana, Hosek Jan, Gregorova Jana, Kos Jiri, Cizek Alois, Hricoviniova Zuzana, Jampilek Josef

机构信息

Department of Analytical Chemistry, Faculty of Natural Sciences, Comenius University, Ilkovicova 6, 842 15 Bratislava, Slovakia.

Department of Infectious Diseases and Microbiology, Faculty of Veterinary Medicine, University of Veterinary Sciences Brno, Palackeho 1946/1, 612 42 Brno, Czech Republic.

出版信息

Heliyon. 2024 Apr 2;10(7):e29051. doi: 10.1016/j.heliyon.2024.e29051. eCollection 2024 Apr 15.

DOI:10.1016/j.heliyon.2024.e29051
PMID:38601653
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11004567/
Abstract

A series of nine 2,3-disubstituted-quinazolin-4(3)-one derived Schiff bases and their three Cu(II) complexes was prepared and tested for their antimicrobial activities against reference strains ATCC 29213 and ATCC 29212 and resistant clinical isolates of methicillin-resistant (MRSA) and vancomycin-resistant (VRE). All the substances were tested against HRa ATCC 25177, DSM 44162 and ATCC 700084. While anti-enterococcal and antimycobacterial activities were insignificant, 3-[()-(2-hydroxy-5-nitrobenzylidene)amino]-2-(2-hydroxy-5-nitrophenyl)-2,3-dihydroquinazolin-4(1)-one () and its Cu(II) complex () demonstrated bacteriostatic antistaphylococcal activity. In addition, both compounds, as well as the other two prepared complexes, showed antibiofilm activity, which resulted in a reduction of biofilm formation and eradication of mature biofilm by 80% even at concentrations lower than the values of their minimum inhibitory concentrations. In addition, the compounds were tested for their cytotoxic effect on the human monocytic leukemia cell line THP-1. The antileukemic efficiency was improved by the preparation of Cu(II) complexes from the corresponding non-chelated Schiff base ligands.

摘要

制备了一系列九个2,3 - 二取代喹唑啉 - 4(3) - 酮衍生的席夫碱及其三种铜(II)配合物，并测试了它们对参考菌株ATCC 29213和ATCC 29212以及耐甲氧西林（MRSA）和耐万古霉素（VRE）的耐药临床分离株的抗菌活性。所有物质均针对HRa ATCC 25177、DSM 44162和ATCC 700084进行了测试。虽然抗肠球菌和抗分枝杆菌活性不显著，但3 - [（） - （2 - 羟基 - 5 - 硝基亚苄基）氨基] - 2 - （2 - 羟基 - 5 - 硝基苯基） - 2,3 - 二氢喹唑啉 - 4(1) - 酮（）及其铜(II)配合物（）表现出抑菌性抗葡萄球菌活性。此外，这两种化合物以及另外两种制备的配合物均显示出抗生物膜活性，即使在浓度低于其最低抑菌浓度值时，也能使生物膜形成减少并使成熟生物膜根除80%。此外，还测试了这些化合物对人单核细胞白血病细胞系THP - 1的细胞毒性作用。由相应的非螯合席夫碱配体制备铜(II)配合物可提高抗白血病效率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/8df404b869ad/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/5ef4e2b64d8f/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/9d6926b226c7/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/1dbe35908859/sc2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/df86f3006947/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/7b8112ffa806/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/5bfb95841bc3/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/8df404b869ad/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/5ef4e2b64d8f/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/9d6926b226c7/sc1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/1dbe35908859/sc2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/df86f3006947/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/7b8112ffa806/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/5bfb95841bc3/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55e6/11004567/8df404b869ad/gr4.jpg

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Dual Anticancer and Antibacterial Properties of Silica-Based Theranostic Nanomaterials Functionalized with Coumarin343, Folic Acid and a Cytotoxic Organotin(IV) Metallodrug.用香豆素343、叶酸和一种细胞毒性有机锡（IV）金属药物功能化的基于二氧化硅的诊疗纳米材料的双重抗癌和抗菌特性
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喹唑酮，药物研发的制胜之选。
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