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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents.
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Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents.

机译：合成新的4-氨基喹啉和喹啉ac啶杂化物作为抗疟剂。

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摘要

Despite emergence of resistance to CQ and other 4-aminoquinoline drugs in most of the endemic regions, research findings provide considerable support that there is still significant potential to discover new affordable, safe, and efficacious 4-aminoquinoline antimalarials. In present study, new side chain modified 4-aminoquinoline derivatives and quinoline-acridine hybrids were synthesized and evaluated in vitro against NF 54 strain of Plasmodium falciparum. Among the evaluated compounds, compound 17 (MIC=0.125 mug/mL) was equipotent to standard drug CQ (MIC=0.125 mug/mL) and compound 21 (MIC=0.031 mug/mL) was four times more potent than CQ. Compound 17 showed the curative response to all the treated swiss mice infected with CQ-resistant N-67 strain of Plasmodium yoelii at the doses 50 mg/kg and 25 mg/kg for four days by intraperitoneal route and was found to be orally active at the dose of 100 mg/kg for four days. The promising antimalarial potency of compound 17 highlights the significance of exploring the privileged 4-aminoquinoline class for new antimalarials.
机译：尽管在大多数流行地区对CQ和其他4-氨基喹啉药物均产生了抗药性，但研究结果提供了可观的支持，即仍有巨大的潜力发现新的负担得起，安全有效的4-氨基喹啉抗疟药。在本研究中，合成了新的侧链修饰的4-氨基喹啉衍生物和喹啉-啶杂化物，并在体外针对恶性疟原虫的NF 54菌株进行了评估。在评估的化合物中，化合物17（MIC = 0.125杯/毫升）与标准药物CQ（MIC = 0.125杯/毫升）等价，化合物21（MIC = 0.031杯/毫升）的效力是CQ的四倍。化合物17通过腹膜内途径对剂量为50 mg / kg和25 mg / kg的经CQ耐药的约氏疟原虫N-67株感染的所有治疗过的瑞士小鼠经腹膜内途径表现出治疗反应，持续4天。 100 mg / kg的剂量持续4天。化合物17的有希望的抗疟药效力突出了探索特权4-氨基喹啉类用于新抗疟药的重要性。

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