Department of Chemical Sciences, Universiti Kebangsaan Malaysia (UKM), Bangi, 43600, Selangor, Malaysia.
Department of Radiology, Biomedical Research Imaging Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Eur J Med Chem. 2023 Nov 5;259:115694. doi: 10.1016/j.ejmech.2023.115694. Epub 2023 Jul 29.
Reviewing the advancements in malaria treatment, the emergence of triazole hybrid compounds stands out as a groundbreaking development. Combining the advantages of triazole and other moieties, these hybrid compounds offer a new frontier in the battle against malaria. Their potential as effective antimalarial agents has captured the attention of researchers and holds promise for overcoming the challenges posed by drug-resistant malaria strains. We focused on their broad spectrum of antimalarial activity of diverse hybridized 1,2,3-triazoles and 1,2,4-triazoles, structure-activity relationship (SAR), drug-likeness, bioavailability and pharmacokinetic properties reported since 2018 targeting multiple stages of the Plasmodium life cycle. This versatility makes them highly effective against both drug-sensitive and drug-resistant strains of P. falciparum, making them invaluable tools in regions where resistance is prevalent. The synergistic effects of combining the triazole moiety with other pharmacophores have resulted in even greater antimalarial potency. This approach has the potential to circumvent existing resistance mechanisms and provide a more sustainable solution to malaria treatment. While triazole hybrid compounds show great promise, further research and clinical trials are warranted to fully evaluate their safety, efficacy and long-term effects. As research progresses, these compounds can potentially revolutionize the field and contribute to global efforts to eradicate malaria, ultimately saving countless lives worldwide.
回顾疟疾治疗的进展,三唑杂合化合物的出现是一个开创性的发展。这些杂合化合物结合了三唑和其他部分的优势,为对抗疟疾开辟了新的前沿。它们作为有效抗疟药物的潜力引起了研究人员的关注,并有望克服耐药疟原虫菌株带来的挑战。我们专注于报道自 2018 年以来针对疟原虫生命周期多个阶段的具有广泛抗疟活性的各种杂化 1,2,3-三唑和 1,2,4-三唑、构效关系 (SAR)、类药性、生物利用度和药代动力学特性的三唑杂合化合物。这种多功能性使它们对敏感和耐药的疟原虫菌株都非常有效,使它们成为耐药性流行地区非常有价值的工具。将三唑部分与其他药效团结合的协同效应导致了更强的抗疟效力。这种方法有可能规避现有的耐药机制,并为疟疾治疗提供更可持续的解决方案。虽然三唑杂合化合物显示出巨大的潜力,但仍需要进一步的研究和临床试验来充分评估它们的安全性、疗效和长期效果。随着研究的进展,这些化合物有可能彻底改变该领域,并为全球消除疟疾的努力做出贡献,最终拯救全球无数生命。