The novel ligand, 1-(phthalazin-1(2H)-one)[(pyridin-2-yl)ethylidene]hydrazone,(APN), derived from the antihypertensive drug, hydralazine hydrochloride, was synthesized and characterized by spectroscopic methods (IR, 1...The novel ligand, 1-(phthalazin-1(2H)-one)[(pyridin-2-yl)ethylidene]hydrazone,(APN), derived from the antihypertensive drug, hydralazine hydrochloride, was synthesized and characterized by spectroscopic methods (IR, 1H NMR). The X-ray crystallographic data indicates that APN has an exocyclic C=N bond on the hydralazine moiety. APN revealed significant anti-onchocercal activity with IC50 values of 0.3125 μg/mL on microfilaria and 10 μg/mL on adult worms compared to the standard drug, ivermectin.展开更多
A novel isoflavone–chromone flavonoid C–O–C dimmer,brevipedicelone D(1),along with one new C–O–C biflavonoid derivative,brevipedicelone E(2),were isolated from the ethyl acetate extract of the leaves of Garcinia ...A novel isoflavone–chromone flavonoid C–O–C dimmer,brevipedicelone D(1),along with one new C–O–C biflavonoid derivative,brevipedicelone E(2),were isolated from the ethyl acetate extract of the leaves of Garcinia brevipedicellata,a medicinal plant used in folk medicine in parts of Cameroon.Their structures were elucidated by extensive spectroscopic techniques,including 1D-and 2D-NMR,MS experiments,as well as comparing their spectral data with those of known analogues.Anti-onchocercal screening of 1 showed moderate inhibition of adult worm motility of Onchocerca ochengi by 60%at the highest concentration(20 μg/mL)and inhibited motility of both the juvenile worms of O.ochengi and Loa loa by 90%at this same concentration.展开更多
文摘The novel ligand, 1-(phthalazin-1(2H)-one)[(pyridin-2-yl)ethylidene]hydrazone,(APN), derived from the antihypertensive drug, hydralazine hydrochloride, was synthesized and characterized by spectroscopic methods (IR, 1H NMR). The X-ray crystallographic data indicates that APN has an exocyclic C=N bond on the hydralazine moiety. APN revealed significant anti-onchocercal activity with IC50 values of 0.3125 μg/mL on microfilaria and 10 μg/mL on adult worms compared to the standard drug, ivermectin.
基金Mirabel Akongwi gratefully acknowledges sup-port by the ministry of higher education of Cameroon(MINESUP)for financial support.
文摘A novel isoflavone–chromone flavonoid C–O–C dimmer,brevipedicelone D(1),along with one new C–O–C biflavonoid derivative,brevipedicelone E(2),were isolated from the ethyl acetate extract of the leaves of Garcinia brevipedicellata,a medicinal plant used in folk medicine in parts of Cameroon.Their structures were elucidated by extensive spectroscopic techniques,including 1D-and 2D-NMR,MS experiments,as well as comparing their spectral data with those of known analogues.Anti-onchocercal screening of 1 showed moderate inhibition of adult worm motility of Onchocerca ochengi by 60%at the highest concentration(20 μg/mL)and inhibited motility of both the juvenile worms of O.ochengi and Loa loa by 90%at this same concentration.
