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Novel Hydralazine Schif. Base Derivatives and Their Antimicrobial, Antioxidant and Antiplasmodial Properties

International Journal of.Organic Chemistry 2020年第1期10卷 1-16页

作者： angelbert f. awantu Yannick Stephane f. f.ngang Godf.ed A. Ayimele Edouard A. Nantia Patrick V. T. f.kou f.brice f. Boyom Celine K. Ngwang Bruno N. Lenta Silvère A. Ngouela Department of.Chemistry The University of Bamenda Bambili Cameroon Department of.Chemistry University of Maroua Maroua Cameroon Department of.Chemistry University of Buea Buea Cameroon Department of.Biochemistry The University of Bamenda Bambili Cameroon Department of.Biochemistry University of Yaoundé I Yaoundé Cameroon Department of.Chemistry Higher Teachers’ Training College University of Yaoundé I Yaoundé Cameroon Department of.Organic Chemistry Faculty of Science University of Yaoundé I Yaoundé Cameroon

Two novel Schif. 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 f.om hydralazine hydrochloride, an ef.ective drug against hypertension, were synthesized and characterized by spectroscopic methods, Inf.ared (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 f.rric 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 ef.ect 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 f.r the dose-response studies.

关键词： Hydralazine Hydrochloride Schif. Bases Antimicrobial Anti-Oxidant Anti-Plasmodial Activities

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Synthesis, Molecular Structure, Anti-Plasmodial, Antimicrobial and Anti-Oxidant Screening of.(E)-1-(Phthalazin-1-yl)-1-[(Pyridin-2-yl)Ethylidene]Hydralazine and 1-[2-(1-(pyridine-3- yl)ethylidene)hydrazinyl]phthalazine

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International Journal of.Organic Chemistry 2021年第3期11卷 91-105页

作者： angelbert f. awantu Godf.ed A. Ayimele Jean Jules K. Bankeu Edouard A. Nantia Patrick V. T. f.kou f.brice f. Boyom Emmanuel N. Nf.r Bruno N. Lenta Silvère A. Ngouela Department of.Chemistry The University of Bamenda Bambili Cameroon Department of.Chemistry University of Buea Buea Cameroon Department of.Biochemistry The University of Bamenda Bambili Cameroon Department of.Biochemistry University of Yaoundé I Yaoundé Cameroon Department of.Chemistry Higher Teachers’ Training College University of Yaoundé I Yaoundé Cameroon Department of.Organic Chemistry Faculty of Science University of Yaoundé I Yaoundé Cameroon

Two new hydralazine hydrochloride-derived Schif. bases: (E)-1-(Phthalazin- 1-yl)-1-[(Pyridin-2-yl)Ethylidene]Hydralazine (PPEH), and 1-[2-(1-(pyridine- 3-yl)ethylidene)hydrazinyl]phthalazine (PEHP), were synthesized and partially characterized by spectroscopic and crystallographic methods including IR and X-ray. The single-crystal X-ray diffraction (SCXRD) analysis of PEHP indicates that the hydralazine moiety of both ligands possesses the exocyclic C=N bond. Both, PPEH and PEHP were tested as antimicrobials and antiparasites. Just PEHP could be considered as slightly antiplasmodial and antibacterial agent. In effect, PPEH showed low antimicrobial activity against one bacterial strain with Minimum Inhibitory Concentration (MIC) value of 250 μg/ml while PEHP showed very interesting activity against 18 out of 19 bacterial strains with MIC of 31.25 - 250 μg/ml compared to the standard drug, amoxicillin. PPEH and PEHP showed higher reducing activity on ferric ions compared to Vitamin C. On the other hand, both hidrazaline synthetized derivatives showedf.nt-f.mily:Verdana;"> as better reducing agents than Vitamin C on f.rric io

关键词： Schif. Base Hydralazine Hydrochloride Anti-Plasmodial Activity Antimicrobial Activity Anti-Oxidant Activity

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