The antimalarial activity of Ru-chloroquine complexes against resistant Plasmodium falciparum is related to lipophilicity, basicity, and heme aggregation inhibition ability near water/n-octanol interfaces.
The antimalarial activity of Ru-chloroquine complexes against resistant Plasmodium falciparum is related to lipophilicity, basicity, and heme aggregation inhibition ability near water/n-octanol interfaces.
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DOI：
10.1007/s00775-009-0498-4
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发表时间：
2009-08
影响因子：
3
通讯作者：
Sanchez-Delgado, Roberto A.
中科院分区：
文献类型：
--
作者：
Martinez, Alberto;Rajapakse, Chandima S. K.;Jalloh, Dalanda;Dautriche, Cula;Sanchez-Delgado, Roberto A.
我们测量了最近报道的一系列钌- π芳烃-氯喹（CQ）配合物的水/正辛醇分配系数、pKa值、血红素结合常数和血红素聚集抑制活性，这些配合物对恶性疟原虫抗CQ菌株有活性。测量水/正辛醇界面附近金属配合物的血红素聚集抑制活性，定性预测其对抗性寄生虫的抗疟原虫作用，与CQ有关；我们得出结论，这种改进的方法可能比在酸性缓冲液中进行的标准测试更能预测抗疟效力。从我们的数据中出现了一些有趣的趋势，表明抗疟原虫活性与所研究化合物的亲脂性、碱性和结构细节相关的效应平衡有关。
We have measured water/n-octanol partition coefficients, pKa values, heme binding constants, and heme aggregation inhibition activity of a series of ruthenium–πarene–chloroquine (CQ) complexes recently reported to be active against CQ-resistant strains of Plasmodium falciparum. Measurements of heme aggregation inhibition activity of the metal complexes near water/n-octanol interfaces qualitatively predict their superior antiplasmodial action against resistant parasites, in relation to CQ; we conclude that this modified method may be a better predictor of antimalarial potency than standard tests in aqueous acidic buffer. Some interesting tendencies emerge from our data, indicating that the antiplasmodial activity is related to a balance of effects associated with the lipophilicity, basicity, and structural details of the compounds studied.
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影响因子：
3
作者：
Warhurst DC
通讯作者：
Warhurst DC
影响因子：
3.9
作者：
Egan, TJ;Mavuso, WW;Marques, HM
通讯作者：
Marques, HM
影响因子：
4.9
作者：
Biot, Christophe;Taramelli, Donatella;Egan, Timothy J.
通讯作者：
Egan, Timothy J.
影响因子：
2.9
作者：
Rappel, C;Galanski, M;Keppler, BK
通讯作者：
Keppler, BK
影响因子：
3.5
作者：
Egan, Timothy J.;Chen, Jeff Y-J.;Wood, Bayden R.
通讯作者：
Wood, Bayden R.