{"title":"抗疟分子最新进展综述:合成方法和SAR研究。","authors":"Hamna Nawaz, Ayesha Malik, Nasir Rasool, Aqsa Kanwal, Tahira Khalid, Iffat Almas, Samreen Gul Khan","doi":"10.1007/s11030-025-11143-4","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":708,"journal":{"name":"Molecular Diversity","volume":" ","pages":""},"PeriodicalIF":3.9000,"publicationDate":"2025-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"An updated survey on the recent advancement of antimalarial molecules: synthetic methodologies and SAR studies.\",\"authors\":\"Hamna Nawaz, Ayesha Malik, Nasir Rasool, Aqsa Kanwal, Tahira Khalid, Iffat Almas, Samreen Gul Khan\",\"doi\":\"10.1007/s11030-025-11143-4\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":708,\"journal\":{\"name\":\"Molecular Diversity\",\"volume\":\" \",\"pages\":\"\"},\"PeriodicalIF\":3.9000,\"publicationDate\":\"2025-03-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molecular Diversity\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1007/s11030-025-11143-4\",\"RegionNum\":2,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, APPLIED\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Diversity","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1007/s11030-025-11143-4","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
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.
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;