抗疟分子最新进展综述:合成方法和SAR研究。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Hamna Nawaz, Ayesha Malik, Nasir Rasool, Aqsa Kanwal, Tahira Khalid, Iffat Almas, Samreen Gul Khan
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引用次数: 0

摘要

疟疾病例不断增加是一个严重的全球健康问题,也是死亡率上升的主要原因。受感染的蚊子传播以疟原虫为基础的疾病。抗疟药物发现的最新进展集中在开发具有独特作用机制的新分子以对抗这种日益增长的耐药性。本文综述了合成混合抗疟化合物的最新发现,这些化合物结合不同的药效团来增强治疗效果,从而产生对氯喹、奎宁和青蒿素耐药/敏感菌株都有强效作用的化合物。值得注意的是,不同支架的结合,如1,2,4-三氧嘧啶、卤化喹啉、吡唑啉和磺胺类化合物,已经产生了有希望的候选物,不仅表现出高效力,而且对药物开发和新靶点的探索具有良好的药代动力学特征。本综述重点介绍了2019-2024年在鉴定和合成杂交抗疟疾分子方面取得的进展,同时解决了该领域存在的挑战。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
An updated survey on the recent advancement of antimalarial molecules: synthetic methodologies and SAR studies.

An ongoing escalation in malaria cases is a critical global health issue and also a leading source of increased mortality rates. Infected mosquitos spread the Plasmodium parasite-based disease,. Recent advancements in antimalarial drug discovery have focused on developing novel molecules with unique mechanisms of action to combat this growing resistance. This review focuses on the latest findings in synthesizing hybrid antimalarial compounds, which combine different pharmacophores to enhance therapeutic efficacy, resulting in compounds that exhibit potent action against both resistant/sensitive strains of chloroquine, quinine, and artemisinin. Notably, the incorporation of diverse scaffolds such as 1,2,4-trioxanes, halogenated quinolines, pyrazoline, and sulfonamides has led to promising candidates that not only demonstrate high potency but also favorable pharmacokinetic profiles for drug development, the exploration of novel targets. This review highlights the progress (2019-2024) made in identifying and synthesizing hybrid antimalarial molecules while addressing existing challenges in the field.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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