Two new hydralazine hydrochloride-derived Schiff bases</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">:</span></span><span style="...Two new hydralazine hydrochloride-derived Schiff bases</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">:</span></span><span style="font-family:Verdana;"> (E)-1-(Phthalazin-</span><span style="font-family:Verdana;"> </span><span style="font-family:Verdana;">1-yl)-1-[(Pyridin-2-yl)Ethylidene]Hydralazine (PPEH), and 1-[2-(1-(pyridine-</span><span style="font-family:Verdana;"> </span><span style="font-family:Verdana;">3</span><span style="font-family:Verdana;">-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 indicate</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">s</span></span><span style="font-family:Verdana;"> that the hydralazine moiety of both ligands possess</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">es</span></span><span style="font-family:Verdana;"> the exoc</span><span style="font-family:Verdana;">yclic 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 </span><span style="font-family:Verdana;"><span style="font-family:Verdana;">-</span></span><span style="font-family:Verdana;"> 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 show</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">ed</span></span><span style="font-family:Verdana;"> as better reducing agents than Vitamin C on ferric ions, while again, only the PEHP show</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">ed</span></span><span style="font-family:Verdana;"> slightly high inhibition of lipid peroxidation using Vitamin C as standard. Regarding their catalase activity, both compounds show</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">ed</span></span><span style="font-family:Verdana;"> concentration dependent effect, but Vitamin C continued showing a higher stimulatory effect on the enzyme activity. Additionally, while PPEH showed less than 80% inhibition in the preliminary antiplasmodial assay and so was not considered for the dose-response studies, PEHP</span><span style="font-family:Verdana;"> displayed an inhibition percentage of 83.60% and 50% Inhibitory Concentration (IC</span><sub><span style="font-family:Verdana;vertical-align:sub;">50</span></sub><span style="font-family:Verdana;">) value of 44.13 μg/mL compared to the standard drug, artemisinin and was classified as slightly active</span><span style="font-family:Verdana;">.展开更多
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 hyp...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.展开更多
文摘Two new hydralazine hydrochloride-derived Schiff bases</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">:</span></span><span style="font-family:Verdana;"> (E)-1-(Phthalazin-</span><span style="font-family:Verdana;"> </span><span style="font-family:Verdana;">1-yl)-1-[(Pyridin-2-yl)Ethylidene]Hydralazine (PPEH), and 1-[2-(1-(pyridine-</span><span style="font-family:Verdana;"> </span><span style="font-family:Verdana;">3</span><span style="font-family:Verdana;">-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 indicate</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">s</span></span><span style="font-family:Verdana;"> that the hydralazine moiety of both ligands possess</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">es</span></span><span style="font-family:Verdana;"> the exoc</span><span style="font-family:Verdana;">yclic 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 </span><span style="font-family:Verdana;"><span style="font-family:Verdana;">-</span></span><span style="font-family:Verdana;"> 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 show</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">ed</span></span><span style="font-family:Verdana;"> as better reducing agents than Vitamin C on ferric ions, while again, only the PEHP show</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">ed</span></span><span style="font-family:Verdana;"> slightly high inhibition of lipid peroxidation using Vitamin C as standard. Regarding their catalase activity, both compounds show</span><span style="font-family:Verdana;"><span style="font-family:Verdana;">ed</span></span><span style="font-family:Verdana;"> concentration dependent effect, but Vitamin C continued showing a higher stimulatory effect on the enzyme activity. Additionally, while PPEH showed less than 80% inhibition in the preliminary antiplasmodial assay and so was not considered for the dose-response studies, PEHP</span><span style="font-family:Verdana;"> displayed an inhibition percentage of 83.60% and 50% Inhibitory Concentration (IC</span><sub><span style="font-family:Verdana;vertical-align:sub;">50</span></sub><span style="font-family:Verdana;">) value of 44.13 μg/mL compared to the standard drug, artemisinin and was classified as slightly active</span><span style="font-family:Verdana;">.
文摘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.