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Therefore, there is an urgent need to discover and develop new antiplasmodial candidates. In this work, we present a novel strategy to develop a multitarget metallic hybrid antimalarial agent with possible dual efficacy in both sexual and asexual erythrocytic stages. A hybrid of antimalarial drugs (chloroquine and primaquine) linked by gold(I) was synthesized and characterized by spectroscopic and analytical techniques. The CQPQ\u2010gold(I) hybrid molecule affects essential parasite targets, it inhibits \u03b2\u2010hematin formation and interacts moderately with the DNA minor groove. Its interaction with PfTrxR was also examined in computational modeling studies. The CQPQ\u2010gold(I) hybrid displayed an excellent <jats:italic>in\u2005vitro<\/jats:italic> antimalarial activity against the blood\u2010stage of <jats:italic>Plasmodium falciparum<\/jats:italic> and liver\u2010stage of <jats:italic>Plasmodium berghei<\/jats:italic> and efficacy <jats:italic>in\u2005vivo<\/jats:italic> against <jats:italic>P. berghei<\/jats:italic>, thereby demonstrating its multiple\u2010stage antiplasmodial activity. This metallic hybrid is a promising chemotherapeutic agent that could act in the treatment, prevention, and transmission of malaria.<\/jats:p>","DOI":"10.1002\/cmdc.202000653","type":"journal-article","created":{"date-parts":[[2020,11,24]],"date-time":"2020-11-24T22:36:39Z","timestamp":1606257399000},"page":"662-678","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":26,"title":["A Novel Hybrid of Chloroquine and Primaquine Linked by Gold(I): Multitarget and Multiphase Antiplasmodial Agent"],"prefix":"10.1002","volume":"16","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-5109-253X","authenticated-orcid":false,"given":"Caroline","family":"de Souza Pereira","sequence":"first","affiliation":[{"name":"Departamento de Qu\u00edmica Universidade Federal de Juiz de Fora, Rua Jos\u00e9 Louren\u00e7o Kelmer  s\/n \u2013 Campus Universit\u00e1rio Bairro Martelos CEP 36036-900 Juiz de Fora, Minas Gerais Brasil"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7191-4809","authenticated-orcid":false,"given":"Helenita","family":"Costa Quadros","sequence":"additional","affiliation":[{"name":"Instituto Gon\u00e7alo Moniz  Funda\u00e7\u00e3o Oswaldo Cruz, Av. 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