Recent developments in antimalarial drug discovery

IF 3.3 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Bioorganic & Medicinal Chemistry Pub Date : 2023-06-06 DOI:10.1016/j.bmc.2023.117339
Théoneste Umumararungu , Jean Bosco Nkuranga , Gratien Habarurema , Jean Baptiste Nyandwi , Marie Jeanne Mukazayire , Janvier Mukiza , Raymond Muganga , Innocent Hahirwa , Matabishi Mpenda , Alain Nyirimigabo Katembezi , Emmanuel Oladayo Olawode , Egide Kayitare , Pierre Claver Kayumba
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引用次数: 1

Abstract

Although malaria remains a big burden to many countries that it threatens their socio-economic stability, particularly in the countries where malaria is endemic, there have been great efforts to eradicate this disease with both successes and failures. For example, there has been a great improvement in malaria prevention and treatment methods with a net reduction in infection and mortality rates. However, the disease remains a global threat in terms of the number of people affected because it is one of the infectious diseases that has the highest prevalence rate, especially in Africa where the deadly Plasmodium falciparum is still widely spread. Methods to fight malaria are being diversified, including the use of mosquito nets, the target candidate profiles (TCPs) and target product profiles (TPPs) of medicine for malarial venture (MMV) strategy, the search for newer and potent drugs that could reverse chloroquine resistance, and the use of adjuvants such as rosiglitazone and sevuparin. Although these adjuvants have no antiplasmodial activity, they can help to alleviate the effects which result from plasmodium invasion such as cytoadherence. The list of new antimalarial drugs under development is long, including the out of ordinary new drugs MMV048, CDRI-97/78 and INE963 from South Africa, India and Novartis, respectively.

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抗疟药物发现的最新进展
虽然疟疾仍然是许多国家的一大负担,威胁着它们的社会经济稳定,特别是在疟疾流行的国家,但为根除这一疾病作出了巨大努力,既有成功,也有失败。例如,疟疾的预防和治疗方法有了很大改进,感染和死亡率净下降。然而,就受影响人数而言,这种疾病仍然是全球威胁,因为它是流行率最高的传染病之一,特别是在致命的恶性疟原虫仍然广泛传播的非洲。抗击疟疾的方法正在多样化,包括使用蚊帐、疟疾风险药物(MMV)战略的候选靶标谱(TCPs)和靶标产品谱(TPPs)、寻找能够逆转氯喹耐药性的新型强效药物,以及使用罗格列酮和sevuparin等佐剂。虽然这些佐剂没有抗疟原虫活性,但它们可以帮助减轻由疟原虫入侵引起的影响,如细胞粘附。正在开发的抗疟新药清单很长,包括来自南非、印度和诺华公司的不同寻常的新药MMV048、cdr -97/78和INE963。
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来源期刊
Bioorganic & Medicinal Chemistry
Bioorganic & Medicinal Chemistry 医学-生化与分子生物学
CiteScore
6.80
自引率
2.90%
发文量
413
审稿时长
17 days
期刊介绍: Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.
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