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4(1H)-quinolones having antimalarial activity with reduced chemical resistance

机译:具有抗疟疾活性和降低的化学抗性的4(1H)-喹诺酮类

摘要

Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.
机译:提供了4(1H)-喹诺酮衍生物,其有效地抑制或消除了疟原虫生命周期中至少一个阶段的活力,并显示出降低的诱导目标寄生虫对化合物产生抗性的倾向。特别地,化合物可以是苯氧基乙氧基-喹诺酮的衍生物,并且包括但不仅限于7-(2-苯氧基乙氧基)喹啉衍生物。这些化合物可以自己与至少一种其他衍生物化合物或与其他抗疟疾化合物一起施用于动物或人类受试者。可以配制治疗组合物以减少接受受试者中 Plasmodium 的感染程度,或降低给药后 Plasmodium 感染的发生或建立的可能性。在寄生虫接触对象之前。可以配制治疗组合物以提供有效的单剂量抗疟化合物或在一段时间内多次给药。

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