{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Basilico N"],"funding":["A*STAR Infectious Disease labs","Global Health Program of the Bill &amp;amp; Melinda Gates Foundation","6th Framework Programme of the European Community","orizontal Programme on Infectious Diseases under the Agency for Science, Technology and Research","SMRU supported by The Wellcome Trust of Great Britain","Ministero dell’Istruzione, dell’Università e della Ricerca (PRIN) Projects","Ministero degli Affari Esteri e della Cooperazione Internazionale","Wellcome Trust"],"pagination":["836"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC10216263"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["13(5)"],"pubmed_abstract":["The 4-aminoquinoline drugs, such as chloroquine (CQ), amodiaquine or piperaquine, are still commonly used for malaria treatment, either alone (CQ) or in combination with artemisinin derivatives. We previously described the excellent in vitro activity of a novel pyrrolizidinylmethyl derivative of 4-amino-7-chloroquinoline, named <b>MG3,</b> against <i>P. falciparum</i> drug-resistant parasites. Here, we report the optimized and safer synthesis of <b>MG3</b>, now suitable for a scale-up, and its additional in vitro and in vivo characterization. <b>MG3</b> is active against a panel of <i>P. vivax</i> and <i>P. falciparum</i> field isolates, either alone or in combination with artemisinin derivatives. In vivo <b>MG3</b> is orally active in the <i>P. berghei, P. chabaudi,</i> and <i>P. yoelii</"],"journal":["Biomolecules"],"pubmed_title":["Favorable Preclinical Pharmacological Profile of a Novel Antimalarial Pyrrolizidinylmethyl Derivative of 4-amino-7-chloroquinoline with Potent In Vitro and In Vivo Activities."],"pmcid":["PMC10216263"],"funding_grant_id":["2010C2LKKJ_006","OPP1040394","PGR00949","20154JRJPP_004","IP-018834"],"pubmed_authors":["Dondio G","Renia L","Nasser S","D'Alessandro S","Nosten F","Vivas L","Suwanarusk R","Misiano P","Russell BM","Romeo S","Yardley V","Taramelli D","Basilico N","Sparatore A","Parapini S"],"additional_accession":[]},"is_claimable":false,"name":"Favorable Preclinical Pharmacological Profile of a Novel Antimalarial Pyrrolizidinylmethyl Derivative of 4-amino-7-chloroquinoline with Potent In Vitro and In Vivo Activities.","description":"The 4-aminoquinoline drugs, such as chloroquine (CQ), amodiaquine or piperaquine, are still commonly used for malaria treatment, either alone (CQ) or in combination with artemisinin derivatives. We previously described the excellent in vitro activity of a novel pyrrolizidinylmethyl derivative of 4-amino-7-chloroquinoline, named <b>MG3,</b> against <i>P. falciparum</i> drug-resistant parasites. Here, we report the optimized and safer synthesis of <b>MG3</b>, now suitable for a scale-up, and its additional in vitro and in vivo characterization. <b>MG3</b> is active against a panel of <i>P. vivax</i> and <i>P. falciparum</i> field isolates, either alone or in combination with artemisinin derivatives. In vivo <b>MG3</b> is orally active in the <i>P. berghei, P. chabaudi,</i> and <i>P. yoelii</","dates":{"release":"2023-01-01T00:00:00Z","publication":"2023 May","modification":"2026-04-08T03:19:34.545Z","creation":"2025-04-07T00:27:20.922Z"},"accession":"S-EPMC10216263","cross_references":{"pubmed":["37238706"],"doi":["10.3390/biom13050836"]}}