{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,1]],"date-time":"2025-10-01T18:08:02Z","timestamp":1759342082209,"version":"3.37.3"},"reference-count":0,"publisher":"Bentham Science Publishers Ltd.","issue":"8","funder":[{"DOI":"10.13039\/501100004901","name":"Funda\u00e7\u00e3o de Amparo \u00e0 Pesquisa do Estado de Minas Gerais","doi-asserted-by":"publisher","award":["APQ-0120917-17"],"award-info":[{"award-number":["APQ-0120917-17"]}],"id":[{"id":"10.13039\/501100004901","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100003593","name":"Conselho Nacional de Desenvolvimento Cient\u00edfico e Tecnol\u00f3gico","doi-asserted-by":"publisher","award":["140335\/2018-8"],"award-info":[{"award-number":["140335\/2018-8"]}],"id":[{"id":"10.13039\/501100003593","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["MC"],"published-print":{"date-parts":[[2021,9,10]]},"abstract":"<jats:sec>\n<jats:title>Background:<\/jats:title>\n<jats:p>Malaria greatly affects the world health, having caused more than 228 million\ncases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating\nthe need for the development of new antimalarial drugs.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Objective:<\/jats:title>\n<jats:p>Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins\nand a 3,4-dihydroisocoumarin.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Methods:<\/jats:title>\n<jats:p>The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole\nring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-\ndihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented\nconnection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products\nwere tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant\nand sensitive strains (W2 and 3D7, respectively).<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Results:<\/jats:title>\n<jats:p>Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of\n25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89\n\u03bcM and 0.85-2.07 \u03bcM against W2 and 3D7 strains, respectively.<\/jats:p>\n<\/jats:sec>\n<jats:sec>\n<jats:title>Conclusion:<\/jats:title>\n<jats:p>This study demonstrated the great potential of isocoumarin or 3,4-dihydroisocoumarin derivatives\nbecause practically all the tested substances were active against Plasmodium falciparum.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1573406416666200602161047","type":"journal-article","created":{"date-parts":[[2020,6,2]],"date-time":"2020-06-02T18:29:40Z","timestamp":1591122580000},"page":"820-833","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Synthesis of Novel 1,2,3-Triazole Derivatives of Isocoumarins and 3,4-Dihydroisocoumarin with Potential Antiplasmodial Activity In Vitro"],"prefix":"10.2174","volume":"17","author":[{"given":"Lucas","family":"da Silva Santos","sequence":"first","affiliation":[{"name":"Laboratorio de Sintese Organica (LabSintO), Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Matheus Fillipe Langanke","family":"de Carvalho","sequence":"additional","affiliation":[{"name":"Laboratorio de Sintese Organica (LabSintO), Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ana Claudia","family":"de Souza Pinto","sequence":"additional","affiliation":[{"name":"Nucleo de Pesquisa em Quimica Biologica (NQBio), Universidade Federal de Sao Joao del-Rei - Campus Centro Oeste, Divinopolis, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Amanda Luisa","family":"da Fonseca","sequence":"additional","affiliation":[{"name":"Nucleo de Pesquisa em Quimica Biologica (NQBio), Universidade Federal de Sao Joao del-Rei - Campus Centro Oeste, Divinopolis, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Julio C\u00e9sar","family":"Dias Lopes","sequence":"additional","affiliation":[{"name":"Laboratorio de Sintese Organica (LabSintO), Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Fernando","family":"de Pilla Varotti","sequence":"additional","affiliation":[{"name":"Nucleo de Pesquisa em Quimica Biologica (NQBio), Universidade Federal de Sao Joao del-Rei - Campus Centro Oeste, Divinopolis, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rossimiriam Pereira","family":"de Freitas","sequence":"additional","affiliation":[{"name":"Laboratorio de Sintese Organica (LabSintO), Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rosemeire Brondi","family":"Alves","sequence":"additional","affiliation":[{"name":"Laboratorio de Sintese Organica (LabSintO), Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"965","container-title":["Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/eurekaselect.com\/article\/download\/182454","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/www.eurekaselect.com\/182454\/article","content-type":"text\/html","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/eurekaselect.com\/article\/download\/182454","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2021,9,16]],"date-time":"2021-09-16T09:39:34Z","timestamp":1631785174000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.eurekaselect.com\/182454\/article"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2021,9,10]]},"references-count":0,"journal-issue":{"issue":"8","published-print":{"date-parts":[[2021,9,10]]}},"alternative-id":["LiveAll1"],"URL":"https:\/\/doi.org\/10.2174\/1573406416666200602161047","relation":{},"ISSN":["1573-4064"],"issn-type":[{"type":"print","value":"1573-4064"}],"subject":[],"published":{"date-parts":[[2021,9,10]]},"assertion":[{"value":"Peer Reviewed","order":0,"name":"review_status","label":"Review Status","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Single blind","order":1,"name":"review_process","label":"Review Process","group":{"name":"peer_review_details","label":"Peer Review Details"}},{"value":"Checked with iThenticate","order":0,"name":"screening_status","label":"Screening Status","group":{"name":"plagiarism_screening","label":"Plagiarism Screening"}},{"value":"2019-12-23","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2020-03-20","order":1,"name":"revised","label":"Revised","group":{"name":"publication_history","label":"Publication History"}},{"value":"2020-04-20","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2021-09-10","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}