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首页> 外文期刊>Journal of Inorganic Biochemistry: An Interdisciplinary Journal >Characterisation of Synthetic #beta#-haematin and effects of the antimalarial drugs quinidine, halofantrine, desbutylhalofantrine and mefloquine on its formation
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Characterisation of Synthetic #beta#-haematin and effects of the antimalarial drugs quinidine, halofantrine, desbutylhalofantrine and mefloquine on its formation

机译:合成的#beta#-haematin的表征以及抗疟药奎尼丁,氟安定,去丁基氟安定和甲氟喹对其形成的影响

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摘要

Infrared spectroscopy, elemental analysis and X-ray powder diffraction show that the product of 30 min of reaction of haematin in 4.5M acetate, pH 4.5 at 60 deg C is identical to #beta#-haematin prepared in 4.5M acetic acid at 70 deg C overnight (pH 2.6). There is no evidence for formation of haem-acetate complex, which could not be isolated, even from 11.4 M acetate solution. The antimalarial drugs quinidine, halofantrine, desbutylhalofantrine and mefloquine were found to inhibit formation of #beta#-haematin, while 5-, 6- and 8-aminoquinoline and quinoline were found to have no effect. Quinidine was shown to form a complex with ferriprotoporphyrin IX in 40% DMSO with log K=5.02+-0.03. Log K values for halofantrine and desbutylhalofantrine are 5.29 +- 0.02 and 5.15 +- 0.02 respectively (solutions containing 30% acetonitrile in addition to DMSO to solubilise these drugs), which are both stronger than chloroquine under the dame conditions (log K = 4.56 +- 0.02).
机译:红外光谱,元素分析和X射线粉末衍射显示,血红素在4.5M乙酸中的30分钟反应(60℃pH 4.5)下的产物与在4.5M醋酸中在70℃制备的#beta#-血红素反应相同。 C过夜(pH 2.6)。没有证据表明形成血红素乙酸盐复合物,即使从11.4 M乙酸盐溶液中也无法分离出。发现抗疟药奎尼丁,氟丁嘌呤,去丁基氟丁啶和甲氟喹抑制#beta#-haematin的形成,而5-,6-和8-氨基喹啉和喹啉则无作用。已显示奎尼丁与铁原卟啉IX在40%DMSO中形成络合物,log K = 5.02 + -0.03。氟丁胺和去丁基氟丁胺的Log K值分别为5.29 +-0.02和5.15 +-0.02(除DMSO之外还含有30%乙腈的溶液以溶解这些药物),在dame条件下均比氯喹强(log K = 4.56 + -0.02)。

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