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嵌合体杂合药物在治疗疟疾感染方面的进展:概述,特别强调内过氧化物药效团。

Advancement of chimeric hybrid drugs to cure malaria infection: An overview with special emphasis on endoperoxide pharmacophores.

机构信息

Chemical Biology Laboratory, Department of Chemistry, University of Delhi, Delhi 110007, India.

Chemical Biology Laboratory, Department of Chemistry, University of Delhi, Delhi 110007, India.

出版信息

Eur J Med Chem. 2021 Jul 5;219:113408. doi: 10.1016/j.ejmech.2021.113408. Epub 2021 Apr 4.

Abstract

Emergence and spread of Plasmodium falciparum resistant to artemisinin-based combination therapy has led to a situation of haste in the scientific and pharmaceutical communities. Sincere efforts are redirected towards finding alternative chemotherapeutic agents that are capable of combating multidrug-resistant parasite strains. Extensive research yielded the concept of "Chimeric Bitherapy (CB)" which involves the linking of two molecules with individual pharmacological activity and exhibit dual mode of action into a single hybrid molecule. Current research in this field seems to endorse hybrid molecules as the next-generation antimalarial drugs and are more effective compared to the multi-component drugs because of the lower occurrence of drug-drug adverse effects. This review is an attempt to congregate complete survey on endoperoxide based hybrid antiplasmodial molecules that will give glimpse on the future directions for successful development and discovery of useful antimalarial hybrid drugs.

摘要

疟原虫对基于青蒿素的联合疗法的耐药性的出现和传播,导致科学界和制药界出现了匆忙的局面。人们真诚地努力寻找能够对抗多药耐药寄生虫株的替代化学治疗药物。广泛的研究产生了“嵌合双疗法(CB)”的概念,该概念涉及将两种具有个体药理活性并表现出双重作用模式的分子连接到单个混合分子中。该领域的当前研究似乎支持将混合分子作为下一代抗疟药物,并且与多组分药物相比更有效,因为药物-药物不良反应的发生率较低。这篇综述试图对基于过氧化物的混合抗疟分子进行全面调查,为成功开发和发现有用的抗疟混合药物提供未来方向。

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