In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon

In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon
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DOI:
10.1128/aac.47.4.1391-1394.2003
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发表时间:
2003-04-01
影响因子:
4.9
通讯作者:
Ringwald, P
Ringwald, P
中科院分区:
医学2区
文献类型:
--
作者:
Basco, LK;Ringwald, P

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抗氯喹恶性疟原虫的传播需要不断寻找新药。本文报道了国产双喹啉类新药哌喹对103株新鲜的恶性疟原虫临床分离株的体外抗疟活性,并与其它4-氨基喹啉、Mannich碱衍生物和双氢青蒿素进行了比较。喹唑啉对氯喹敏感和氯喹耐药菌株的活性相当(几何平均50%抑制浓度,38.9 nmol/L;范围,7.76 - 78.3 nmol/L)。氯喹与哌喹的疗效相关性较低(r = 0.257,P < 0.05)。这些结果表明,进一步开发哌喹,与双氢青蒿素组合,有望用于氯喹耐药地区的地方病。
The spread of chloroquine-resistant Plasmodium falciparum calls for a constant search for new drugs. The in vitro activity of piperaquine, a new Chinese synthetic drug belonging to the bisquinolines, was evaluated in 103 fresh clinical isolates of P. falciparum in Cameroon, Central Africa, and compared with that of other 4-aminoquinoline and Mannich base derivatives and dihydroartemisinin. Piperaquine was highly active (geometric mean 50% inhibitory concentration, 38.9 nmol/liter; range, 7.76 to 78.3 nmol/liter) and equally active (P > 0.05) against the chloroquine-sensitive and the chloroquine-resistant isolates. There was a significant but low correlation of response between chloroquine and piperaquine (r = 0.257, P < 0.05). These results suggest that further development of piperaquine, in combination with dihydroartemisinin, holds promise for use in chloroquine-resistant regions of endemicity.