Antiplasmodial and leishmanicidal activities of 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives.

Antiplasmodial and leishmanicidal activities of 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives.
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2-Cyano-3-(4-苯基哌嗪-1-羧酰基)Quinoxaline 1,4-二氧化物衍生物的抗血统和利什甘脉活性。

DOI:
10.3390/molecules17089451
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发表时间:
2012-08-07
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Aldana I
Aldana I
中科院分区:
其他
文献类型:
--
作者:
Barea C;Pabón A;Galiano S;Pérez-Silanes S;Gonzalez G;Deyssard C;Monge A;Deharo E;Aldana I

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疟疾和利什曼病是世界上最重要的两种热带寄生虫病。合成了13个新的2-氰基-3-(4-苯基哌嗪-1-氨基)喹恶啉-1,4-二氧化物(CPCQs),并评价了其体外抗恶性疟原虫和无菌婴儿利什曼原虫的活性。还评估了它们对Vero细胞(正常猴肾细胞)的毒性。受试化合物对疟原虫均无有效抑制作用,但其中两个化合物对利什曼原虫表现出较好的抑制活性。对Vero的毒性与利什曼杀伤力有关。
Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Thirteen new 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives (CPCQs) were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against erythrocytic forms of Plasmodium falciparum and axenic forms of Leishmania infantum. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. None of the tested compounds was efficient against Plasmodium, but two of them showed good activity against Leishmania. Toxicity on VERO was correlated with leishmanicidal properties.
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