4,9‐Diaminoacridines and 4‐Aminoacridines as Dual‐Stage Antiplasmodial Hits,ChemMedChem

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4,9‐Diaminoacridines and 4‐Aminoacridines as Dual‐Stage Antiplasmodial Hits
ChemMedChem ( IF 3.6 ) Pub Date : 2020-11-20 , DOI: 10.1002/cmdc.202000740
Mélanie Fonte ₁ , Natália Tassi ₁ , Diana Fontinha ₂ , Inés Bouzón-Arnáiz _{3,

4} , Ricardo Ferraz _{1,

5} , Maria J Araújo ₁ , Xavier Fernàndez-Busquets _{3,

4} , Miguel Prudêncio ₂ , Paula Gomes ₁ , Cátia Teixeira ₁

Affiliation

Multi‐stage drugs have been prioritized in antimalarial drug discovery, as targeting more than one process in the Plasmodium life cycle is likely to increase efficiency, while decreasing the chances of emergence of resistance by the parasite. Herein, we disclose two novel acridine‐based families of compounds that combine the structural features of primaquine and chloroquine. Compounds prepared and studied thus far retained the in vitro activity displayed by the parent drugs against the erythrocytic stages of chloroquine‐sensitive and ‐resistant Plasmodium falciparum strains, and against the hepatic stages of Plasmodium berghei, hence acting as dual‐stage antiplasmodial hits.

中文翻译：

4,9-二氨基吖啶和 4-氨基吖啶作为双阶段抗疟原虫命中

多阶段药物在抗疟药物发现中被优先考虑，因为针对疟原虫生命周期中的一个以上过程可能会提高效率，同时减少寄生虫出现耐药性的机会。在此，我们公开了两种新的基于吖啶的化合物家族，它们结合了伯氨喹和氯喹的结构特征。迄今为止，制备和研究的化合物保留了母体药物对氯喹敏感和耐药恶性疟原虫菌株的红细胞阶段以及伯氏疟原虫肝脏阶段所显示的体外活性，因此作为双阶段抗疟原虫命中。

更新日期：2020-11-20

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