期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 210, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112955
关键词
Clinical candidates; Antimalarials; Drug-resistance; Artemisinin based combination therapy
资金
- University Grants Commission, India
Malaria is an endemic disease prevalent in tropical and subtropical regions, with current therapeutic efforts being insufficient due to drug resistance, lack of vaccine availability, and absence of new mechanism drugs. Recent intensification of antimalarial research has led to the development of single dose multistage therapeutic agents to overcome drug resistance. The review explores progress in developing new promising antimalarials against target proteins with potential for clinical use, along with highlighting drug resistance aspects and new drug candidates.
Malaria is an endemic disease, prevalent in tropical and subtropical regions which cost half of million deaths annually. The eradication of malaria is one of the global health priority nevertheless, current therapeutic efforts seem to be insufficient due to the emergence of drug resistance towards most of the available drugs, even first-line treatment ACT, unavailability of the vaccine, and lack of drugs with a new mechanism of action. Intensification of antimalarial research in recent years has resulted into the development of single dose multistage therapeutic agents which has advantage of overcoming the antimalarial drug resistance. The present review explored the current progress in the development of new promising antimalarials against prominent target proteins that have the potential to be a clinical candidate. Here, we also reviewed different aspects of drug resistance and highlighted new drug candidates that are currently in a clinical trial or clinical development, along with a few other molecules with excellent antimalarial activity overs ACTs. The summarized scientific value of previous approaches and structural features of antimalarials related to the activity are highlighted that will be helpful for the development of next-generation antimalarials. (C) 2020 Elsevier Masson SAS. All rights reserved.
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