盐酸甲氟喹Co(II)配合物的合成、抑菌潜力、抗疟及毒理学活性

Adediji J. Femi, O. J. Ayoola
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引用次数: 4

摘要

采用模板法合成了Co(II)与抗疟药盐酸甲氟喹的过渡金属配合物。化学分析包括电导率测量和光谱研究,提出了配体与金属离子结合的几何形状和模式。从分析数据来看,该配合物的化学计量比为1:1。红外光谱数据还表明,该配体(盐酸甲氟喹)对金属离子表现为具有N:N:O给体序列的三齿配体。该配合物总体呈八面体坐标几何。配合物的10-2 mol dm-3甲醇溶液电导率测定表明配合物具有非电解性质。它还揭示了配体阴离子与配合物是共价键。体内评价抗菌研究的金属配合物显示出更大的活性时,与游离甲氟喹相比。该复合物对疟疾寄生虫(尼日利亚约利疟原虫)进行了筛选:从获得的结果中可以明显看出,与游离的甲氟喹相比,Co(II)甲氟喹具有最高的清除率,可减少约80%的寄生虫病。筛选配体和金属配合物在0.60 mg/Kg体重剂量下对大鼠血清、肝脏和肾脏碱性磷酸酶(ALP)、丙氨酸转氨酶(ALT)和天冬氨酸转氨酶(AST)活性的毒理学活性,每日2次,连用7 d。总的来说,甲氟喹及其金属配合物没有显示出毒性,特别是对肝脏和肾脏。
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Co(II) Complex of Mefloquine Hydrochloride: Synthesis, Antimicrobial Potential, Antimalaria and Toxicological Activities
Transition metal complex of Co(II) with Mefloquine hydrochloride (antimalaria drug) was synthesized using template method. Chemical analysis including conductivity measurements and spectroscopic studies were used to propose the geometry and mode of binding of the ligand to metal ion. From analytical data, the stoichiometry of the complex has been found to be 1:1. Infrared spectral data also suggest that the ligand (mefloquine hydrochloride) behaves as a tridentate ligand with N:N:O donor sequence towards the metal ion. The complex generally showed octahedral coordinate geometry. Conductivity measurement of 10-2 mol dm-3 methanol solution of the complex indicated non-electrolytic nature of metal complex. It also revealed that the ligand anions were covalently bonded to the complex. In-vivo evaluation of antimicrobial studies of the metal complex showed greater activities when compared to the free mefloquine.The complex was screened against malarial parasites (Plasmodium yoelii nigeriensis): It was evident from the results obtained that Co(II) mefloquine has highest clearance of about 80% parasitaemia reduction compared to the free mefloquine. The ligand and metal complex were screened for their toxicological activities at the dose of 0.60 mg/Kg body weight twice daily for seven days on the alkaline phosphatase (ALP), alanine aminotranferase (ALT), and aspartate aminotransferase (AST) activities of rat serum, liver and kidney. Overall, it was revealed that both mefloquine and its metal complex do not showed toxicity particularly on the liver and kidney.
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E-journal of Chemistry
E-journal of Chemistry CHEMISTRY, MULTIDISCIPLINARY-
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