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Antimalarial agents are vital for treating malaria and controlling transmission, and 1,2,4\u2010trioxolane\/trioxane\u2010containing agents, especially artemisinin and its derivatives, own antimalarial efficacy and low toxicity with unique mechanisms of action. Moreover, artemisinin\u2010based combination therapies were recommended by the World Health Organization as the first\u2010line treatment for uncomplicated malaria infection and have remained as the mainstay of the treatment of malaria, demonstrating that 1,2,4\u2010trioxolane\/trioxane derivatives are useful prototypes for the control and eradication of malaria. However, malaria parasites have already developed resistance to almost all of the currently available antimalarial agents, creating an urgent need for the search of novel pharmaceutical interventions for malaria. The purpose of this review article is to provide an emphasis on the current scenario (January 2012 to January 2022) of 1,2,4\u2010trioxolane\/trioxane hybrids and dimers with potential antimalarial activity and the structure\u2013activity relationships are also discussed to facilitate further rational design of more effective candidates.<\/jats:p>","DOI":"10.1002\/ardp.202200077","type":"journal-article","created":{"date-parts":[[2022,4,7]],"date-time":"2022-04-07T03:35:16Z","timestamp":1649302516000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["The antimalarial activity of 1,2,4\u2010trioxolane\/trioxane hybrids and dimers: A review"],"prefix":"10.1002","volume":"355","author":[{"given":"Junman","family":"Fang","sequence":"first","affiliation":[{"name":"College of Life Sciences, Engineering Research Center of the Chinese Ministry of Education for Bioreactor and Pharmaceutical Development Jilin Agricultural University Changchun Jilin China"},{"name":"Shandong Key Laboratory of Biophysics, Institute of Biophysics Dezhou University Dezhou Shandong China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5211-2803","authenticated-orcid":false,"given":"Feng","family":"Song","sequence":"additional","affiliation":[{"name":"Shandong Key Laboratory of Biophysics, Institute of Biophysics Dezhou University Dezhou Shandong China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Fawei","family":"Wang","sequence":"additional","affiliation":[{"name":"College of Life Sciences, Engineering Research Center of the Chinese Ministry of Education for Bioreactor and Pharmaceutical Development Jilin Agricultural University Changchun Jilin China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2022,4,6]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jacc.2020.12.042"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrdp.2017.50"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.jmedchem.9b00761"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.medcli.2020.05.010"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.micpath.2021.105203"},{"key":"e_1_2_7_7_1","doi-asserted-by":"crossref","unstructured":"F. 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