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噻唑和喹啉部分衍生的席夫碱配体的一些金属配合物的合成、表征、抗菌、DNA 切割和体外细胞毒性研究。

Synthesis, characterization, antimicrobial, DNA cleavage, and in vitro cytotoxic studies of some metal complexes of schiff base ligand derived from thiazole and quinoline moiety.

机构信息

Department of Studies and Research in Chemistry, Gulbarga University, GULBARGA, Karnataka 585 106, India.

出版信息

Bioinorg Chem Appl. 2014;2014:314963. doi: 10.1155/2014/314963. Epub 2014 Mar 5.

Abstract

A novel Schiff base ligand N-(4-phenylthiazol-2yl)-2-((2-thiaxo-1,2-dihydroquinolin-3-yl)methylene)hydrazinecarboxamide (L) obtained by the condensation of N-(4-phenylthiazol-2-yl)hydrazinecarboxamide with 2-thioxo-1,2-dihydroquinoline-3-carbaldehyde and its newly synthesized Cu(II), Co(II), Ni(II), and Zn(II) complexes have been characterized by elemental analysis and various spectral studies like FT-IR, (1)H NMR, ESI mass, UV-Visible, ESR, TGA/DTA, and powder X-ray diffraction studies. The Schiff base ligand (L) behaves as tridentate ONS donor and forms the complexes of type [ML(Cl)2] with square pyramidal geometry. The Schiff base ligand (L) and its metal complexes have been screened in vitro for their antibacterial and antifungal activities by minimum inhibitory concentration (MIC) method. The DNA cleavage activity of ligand and its metal complexes were studied using plasmid DNA pBR322 as a target molecule by gel electrophoresis method. The brine shrimp bioassay was also carried out to study the in vitro cytotoxicity properties for the ligand and its metal complexes against Artemia salina. The results showed that the biological activities of the ligand were found to be increased on complexation.

摘要

一种新型的希夫碱配体 N-(4-苯基噻唑-2-基)-2-((2-噻唑并[1,2-a]喹啉-3-基)亚甲基)肼甲酰胺(L)是通过 N-(4-苯基噻唑-2-基)肼甲酰胺与 2-硫代-1,2-二氢喹啉-3-甲醛缩合得到的,其新合成的 Cu(II)、Co(II)、Ni(II)和 Zn(II)配合物已通过元素分析和各种光谱研究(如 FT-IR、(1)H NMR、ESI 质谱、UV-Visible、ESR、TGA/DTA 和粉末 X 射线衍射研究)进行了表征。希夫碱配体(L)作为三齿 ONS 供体,形成具有四方锥几何形状的[ML(Cl)2]类型的配合物。通过最低抑菌浓度(MIC)法,对希夫碱配体(L)及其金属配合物进行了体外抗菌和抗真菌活性筛选。通过凝胶电泳法,用质粒 DNA pBR322 作为靶分子研究了配体及其金属配合物的 DNA 断裂活性。还进行了卤虫生物测定,以研究配体及其金属配合物对 Artemia salina 的体外细胞毒性。结果表明,配体的生物活性在配位后增加。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ea81/3960517/cc4b2a5e8a1b/BCA2014-314963.sch.001.jpg

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