Novel Hydralazine Schiff Base Derivatives and Their Antimicrobial, Antioxidant and Antiplasmodial Properties

A. F. Awantu, Y. Fongang, Godfred A. Ayimele, E. Nantia, P. Fokou, F. Boyom, Celine K. Ngwang, B. Lenta, S. Ngouela
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引用次数: 4

Abstract

Two novel Schiff bases, 3-[1-(2-(phthalazin-1-yl)hydrazono)ethyl)-1,3-oxa- zinane (PHEO) and 2-[(2-(phthalazin-1-yl)hydrazono)methyl]phenol (PHMP), derived from hydralazine hydrochloride, an effective drug against hypertension, were synthesized and characterized by spectroscopic methods, Infrared (IR), Proton Nuclear Magnetic Resonance (1H NMR) and Carbon-13 Nuclear Magnetic Resonance (13C NMR). PHEO showed low antimicrobial activity against one bacterial strain with MIC value of 250 μg/ml while PHMP showed interesting activity against 4 bacterial strains with MIC of 31.25 - 250 μg/ml compared to the standard drug, amoxicillin. PHEO and PHMP showed higher reducing activity on ferric ions compared to Vitamin C. On lipid peroxidation, PHEO showed higher inhibition while PHMP showed lower inhibition compared to Vitamin C. Both compounds presented lower stimulating effect and lower catalase activity compared to the standard Vitamin C. PHEO and PHMP showed less than 80% inhibition in the preliminary antiplasmodial assay and so were not considered for the dose-response studies.
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新型肼嗪席夫碱衍生物及其抗菌、抗氧化和抗等离子体性质
合成了两种新的席夫碱,3-[1-(2-(邻苯二甲嗪-1-基)腙基)乙基)-1,3-氧杂锌烷(PHEO)和2-[(2-(苯二甲肼-1-基)肼基)甲基]苯酚(PHMP),这两种席夫碱来源于抗高血压的有效药物氢肼嗪盐酸盐,并用红外(IR)、质子核磁共振(1H NMR)和碳-13核磁共振(13C NMR)对其进行了表征。与标准药物阿莫西林相比,PHEO对一株MIC值为250μg/ml的菌株表现出较低的抗菌活性,而PHMP对4株MIC为31.25-250μg/ml菌株表现出有趣的抗菌活性。与维生素C相比,PHEO和PHMP对铁离子的还原活性更高。在脂质过氧化方面,PHEO表现出更高的抑制作用,而PHMP表现出更低的抑制作用。与标准维生素C相比。这两种化合物都表现出较低的刺激作用和较低的过氧化氢酶活性。PHEO和PHMP在初步抗疟原虫试验中显示出低于80%的抑制作用,因此不考虑用于剂量反应研究。
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