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合成、光谱和热特性研究铁、锰、铜、钴、镍和锌盐的舒必利配合物。抗菌和抗真菌活性。

Synthesis, spectroscopic and thermal characterization of sulpiride complexes of iron, manganese, copper, cobalt, nickel, and zinc salts. Antibacterial and antifungal activity.

机构信息

Department of Chemistry, Faculty of Science, Cairo University, 12613, Giza, Egypt.

出版信息

Spectrochim Acta A Mol Biomol Spectrosc. 2010 Aug;76(3-4):341-7. doi: 10.1016/j.saa.2010.03.016. Epub 2010 Mar 21.

Abstract

Sulpiride (SPR; L) is a substituted benzamide antipsychotic which is reported to be a selective antagonist of central dopamine receptors and claimed to have mood-elevating properties. The ligation behaviour of SPR drug is studied in order to give an idea about its potentiality towards some transition metals in vitro systems. Metal complexes of SPR have been synthesized by reaction with different metal chlorides. The metal complexes of SPR with the formula [MCl(2)(L)(2)(H(2)O)(2)].nH(2)O [M=Mn(II), Co(II), Ni(II), Cu(II) and Zn(II); n=0-2] and [FeCl(2)(HL)(H(2)O)(3)]Cl.H(2)O have been synthesized and characterized using elemental analysis (CHN), electronic (infrared, solid reflectance and (1)H NMR spectra) and thermal analyses (TG and DTA). The molar conductance data reveal that the bivalent metal chelates are non-electrolytes while Fe(III) complex is 1:1 electrolyte. IR spectra show that SPR is coordinated to the metal ions in a neutral monodentate manner with the amide O. From the magnetic and solid reflectance spectra, octahedral geometry is suggested. The thermal decomposition processes of these complexes were discussed. The correlation coefficient, the activation energies, E*, the pre-exponential factor, A, and the entropies, DeltaS*, enthalpies, DeltaH*, Gibbs free energies, DeltaG*, of the thermal decomposition reactions have been derived from thermogravimetric (TG) and differential thermogravimetric (DTG) curves. The synthesized ligand and its metal complexes were also screened for their antibacterial and antifungal activity against bacterial species (Escherichia coli and Staphylococcus aureus) and fungi (Aspergillus flavus and Candida albicans). The activity data show that the metal complexes are found to have antibacterial and antifungal activity than the parent drug and less than the standard.

摘要

舒必利(SPR;L)是一种取代的苯甲酰胺类抗精神病药,据报道它是中枢多巴胺受体的选择性拮抗剂,并具有改善情绪的特性。研究了 SPR 药物的键合行为,以了解其在体外系统中对一些过渡金属的潜在性。通过与不同的金属氯化物反应合成了 SPR 的金属配合物。SPR 与[MCl 2(L)2(H 2 O)2]。nH 2 O [M=Mn(II),Co(II),Ni(II),Cu(II)和 Zn(II);n=0-2]和[FeCl 2(HL)(H 2 O)(3)]Cl。H 2 O 的金属配合物已通过元素分析(CHN)、电子(红外、固态反射率和(1)H NMR 谱)和热分析(TG 和 DTA)进行了合成和表征。摩尔电导率数据表明,二价金属配合物是非电解质,而 Fe(III)配合物是 1:1 电解质。IR 光谱表明,SPR 以中性单齿方式与酰胺 O 配位到金属离子。根据磁性和固态反射率光谱,建议采用八面体几何形状。讨论了这些配合物的热分解过程。从热重(TG)和差示热重(DTG)曲线得出了这些热分解反应的相关系数、活化能 E*、前指数因子 A 和熵 DeltaS*、焓 DeltaH*、吉布斯自由能 DeltaG*。还对配体及其金属配合物进行了筛选,以评估它们对细菌(大肠杆菌和金黄色葡萄球菌)和真菌(黄曲霉和白色念珠菌)的抗菌和抗真菌活性。活性数据表明,金属配合物的抗菌和抗真菌活性强于母体药物,弱于标准。

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