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Primaquine, an antimalarial 8-aminoquinoline, displays activity against\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Leishmania<\/jats:named-content>\n            spp., and several of its derivatives have been developed as potential antileishmanial drugs. However, primaquine exhibits low oral bioavailability due to oxidative deamination of its aliphatic chain. We previously developed peptidomimetic and organometallic derivatives of primaquine, with higher resistance to proteolytic degradation and oxidative deamination, which presented significant activity against primaquine-sensitive pathogens such as\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Plasmodium<\/jats:named-content>\n            or\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Pneumocystis<\/jats:named-content>\n            . In light of these relevant findings, we decided to evaluate these compounds against both the promastigote and intramacrophagic amastigote forms of\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Leishmania infantum<\/jats:named-content>\n            , the agent of Mediterranean visceral leishmaniasis. We found that several of these compounds had significant activity against\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">L. infantum<\/jats:named-content>\n            . One of the peptidomimetic (3c) and one of the organometallic (7a) derivatives of primaquine were active against the clinically relevant intramacrophagic amastigote form of the parasite, causing &gt;96% reductions in the number of amastigotes per 100 macrophages at 60 and 40 \u03bcM, respectively, while being less cytotoxic for host cells than the reference drugs sitamaquine and miltefosine. Hence, compounds 3c and 7a represent new entries toward the development of new antileishmanial leads.\n          <\/jats:p>","DOI":"10.1128\/aac.00873-12","type":"journal-article","created":{"date-parts":[[2012,8,28]],"date-time":"2012-08-28T02:58:44Z","timestamp":1346122724000},"page":"5774-5781","update-policy":"http:\/\/dx.doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":33,"title":["Peptidomimetic and Organometallic Derivatives of Primaquine Active against Leishmania infantum"],"prefix":"10.1128","volume":"56","author":[{"given":"S\u00edlvia","family":"Vale-Costa","sequence":"first","affiliation":[{"name":"Instituto de Biologia Molecular e Celular, Universidade do Porto, Porto, Portugal"},{"name":"Instituto de Ci\u00eancias Biom\u00e9dicas Abel Salazar, Universidade do Porto, Porto, Portugal"}]},{"given":"Nuno","family":"Vale","sequence":"additional","affiliation":[{"name":"Centro de Investiga\u00e7\u00e3o em Qu\u00edmica, Universidade do Porto, Porto, Portugal"},{"name":"Departamento de Qu\u00edmica e Bioqu\u00edmica, Faculdade de Ci\u00eancias, Universidade do Porto, Porto, Portugal"}]},{"given":"Joana","family":"Matos","sequence":"additional","affiliation":[{"name":"Centro de Investiga\u00e7\u00e3o em Qu\u00edmica, Universidade do Porto, Porto, Portugal"},{"name":"Departamento de Qu\u00edmica e Bioqu\u00edmica, Faculdade de Ci\u00eancias, Universidade do Porto, Porto, Portugal"}]},{"given":"Ana","family":"Tom\u00e1s","sequence":"additional","affiliation":[{"name":"Instituto de Biologia Molecular e Celular, Universidade do Porto, Porto, Portugal"},{"name":"Instituto de Ci\u00eancias Biom\u00e9dicas Abel Salazar, Universidade do Porto, Porto, Portugal"}]},{"given":"Rui","family":"Moreira","sequence":"additional","affiliation":[{"name":"iMed.UL, CECF, Faculdade de Farm\u00e1cia, Universidade de Lisboa, Lisbon, Portugal"}]},{"given":"Paula","family":"Gomes","sequence":"additional","affiliation":[{"name":"Centro de Investiga\u00e7\u00e3o em Qu\u00edmica, Universidade do Porto, Porto, Portugal"},{"name":"Departamento de Qu\u00edmica e Bioqu\u00edmica, Faculdade de Ci\u00eancias, Universidade do Porto, Porto, Portugal"}]},{"given":"Maria Salom\u00e9","family":"Gomes","sequence":"additional","affiliation":[{"name":"Instituto de Biologia Molecular e Celular, Universidade do Porto, Porto, Portugal"},{"name":"Instituto de Ci\u00eancias Biom\u00e9dicas Abel Salazar, Universidade do Porto, Porto, Portugal"}]}],"member":"235","reference":[{"key":"e_1_3_2_2_2","doi-asserted-by":"publisher","DOI":"10.1128\/CMR.00061-07"},{"key":"e_1_3_2_3_2","doi-asserted-by":"crossref","first-page":"888","DOI":"10.1021\/jm0494624","article-title":"Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials","volume":"48","author":"Araujo MJ","year":"2005","unstructured":"AraujoMJ. 2005. 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