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Unfortunately, despite the availability of efficient treatments, we have observed an increase in people infected with malaria since 2015 (from 211 million in 2015 to 229 million in 2019). This trend could partially be due to the development of resistance to all the current drugs. Therefore, there is an urgent need for new alternatives. We have, thus, selected common natural scaffolds, polyhydroxybenzoic acids, and synthesized a library of derivatives to better understand the structure\u2013activity relationships explaining their antiplasmodial effect. Only gallic acid derivatives showed a noticeable potential for further developments. Indeed, they showed a selective inhibitory effect on <jats:italic>Plasmodium<\/jats:italic> (IC<jats:sub>50<\/jats:sub> ~20\u2009\u00b5M, SI\u2009&gt;\u20095) often associated with interesting water solubility. Moreover, this has confirmed the critical importance of free phenolic functions (pyrogallol moiety) for the antimalarial effect. Methyl 4\u2010benzoxy\u20103,5\u2010dihydroxybenzoate (<jats:bold>39<\/jats:bold>) has, for the first time, been recognized as a potential lead for future research because of its marked inhibitory activity against <jats:italic>Plasmodium falciparum<\/jats:italic> and its significant hydrosolubility (3.72\u2009mM).<\/jats:p>","DOI":"10.1002\/ardp.202100190","type":"journal-article","created":{"date-parts":[[2021,8,4]],"date-time":"2021-08-04T07:11:42Z","timestamp":1628061102000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Polyhydroxybenzoic acid derivatives as potential new antimalarial agents"],"prefix":"10.1002","volume":"354","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-6318-4626","authenticated-orcid":false,"given":"Gilles","family":"Degotte","sequence":"first","affiliation":[{"name":"Department of Pharmacy, Laboratory of Medicinal Chemistry, CIRM University of Li\u00e8ge  Li\u00e8ge Belgium"},{"name":"Department of Pharmacy, Laboratory of Pharmacognosy, CIRM University of Li\u00e8ge  Li\u00e8ge Belgium"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8251-8257","authenticated-orcid":false,"given":"Bernard","family":"Pirotte","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Laboratory of Medicinal Chemistry, CIRM University of Li\u00e8ge  Li\u00e8ge Belgium"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0770-9990","authenticated-orcid":false,"given":"Michel","family":"Fr\u00e9d\u00e9rich","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Laboratory of Pharmacognosy, CIRM University of Li\u00e8ge  Li\u00e8ge Belgium"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9252-7798","authenticated-orcid":false,"given":"Pierre","family":"Francotte","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Laboratory of Medicinal Chemistry, CIRM University of Li\u00e8ge  Li\u00e8ge Belgium"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2021,8,4]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1021\/acsinfecdis.9b00371"},{"key":"e_1_2_7_3_1","unstructured":"World Health OrganisationEnding the neglect to attain the sustainable development goals: a road map for neglected tropical diseases 2021\u20132030: overview."},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41586-018-0327-4"},{"key":"e_1_2_7_5_1","unstructured":"World Health Organization 2021 Malaria.https:\/\/www.who.int\/news-room\/fact-sheets\/detail\/malaria"},{"key":"e_1_2_7_6_1","unstructured":"World Health Organization 2019.https:\/\/www.who.int\/news-room\/feature-stories\/detail\/world-malaria-report-2019"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.358.6360.155"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1038\/nature14412"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41591-020-1005-2"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1080\/21645515.2019.1669415"},{"key":"e_1_2_7_11_1","first-page":"337","author":"Pelletier P. 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