{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,9]],"date-time":"2026-03-09T23:33:49Z","timestamp":1773099229659,"version":"3.50.1"},"reference-count":38,"publisher":"American Society for Microbiology","issue":"9","license":[{"start":{"date-parts":[[2015,9,1]],"date-time":"2015-09-01T00:00:00Z","timestamp":1441065600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2015,9]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            The generation of new antileishmanial drugs has become a priority. Selenium and its derivatives stand out as having promising leishmanicidal activity. In fact, some parasites express selenoproteins and metabolize selenium. Recently, selenium derivatives have shown the potential to reduce parasitemia, clinical manifestations, and mortality in parasite-infected mice. In this paper, after selecting four candidates according to drug similarity parameters, we observed that two of them, called compounds 2b [methyl-\n            <jats:italic>N<\/jats:italic>\n            ,\n            <jats:italic>N<\/jats:italic>\n            \u2032-di(thien-2-ylcarbonyl)-imidoselenocarbamate] and 4b [methyl-\n            <jats:italic>N<\/jats:italic>\n            ,\n            <jats:italic>N<\/jats:italic>\n            \u2032-di(5-nitrothien-3-ylcarbonyl)-imidoselenocarbamate], exhibit low 50% inhibitory concentrations (IC\n            <jats:sub>50<\/jats:sub>\n            s) (&lt;3 \u03bcM) and good selectivity indexes (SIs) (&gt;5) in\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">Leishmania major<\/jats:named-content>\n            promastigotes and lack toxicity on macrophages. In addition, in analysis of their therapeutic potential against\n            <jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">L. major<\/jats:named-content>\n            <jats:italic>in vitro<\/jats:italic>\n            infection, both compounds display a dramatic reduction of amastigote burden (\u223c80%) with sublethal concentrations. Furthermore, in macrophages, these selenocompounds induce nitric oxide production, which has been described to be critical for defense against intracellular pathogens. Compounds 2b and 4b were demonstrated to cause cell cycle arrest in G\n            <jats:sub>1<\/jats:sub>\n            . Interestingly, evaluation of expression of genes related to proliferation (PCNA), treatment resistance (ABC transporter and alpha-tubulin), and virulence (quinonoid dihydropteridine reductase [QDPR]) showed several alterations in gene expression profiling. All these results prompt us to propose both compounds as candidates to treat leishmanial infections.\n          <\/jats:p>","DOI":"10.1128\/aac.00997-15","type":"journal-article","created":{"date-parts":[[2015,7,7]],"date-time":"2015-07-07T02:29:57Z","timestamp":1436236197000},"page":"5705-5713","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":29,"title":["Leishmanicidal Activities of Novel Methylseleno-Imidocarbamates"],"prefix":"10.1128","volume":"59","author":[{"given":"Celia","family":"Fern\u00e1ndez-Rubio","sequence":"first","affiliation":[{"name":"Instituto de Salud Tropical (ISTUN), University of Navarra, Pamplona, Spain"},{"name":"Department of Microbiology and Parasitology, University of Navarra, IdiSNA, Navarra Institute for Health Research, Pamplona, Spain"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Daphne","family":"Campbell","sequence":"additional","affiliation":[{"name":"Instituto de Salud Tropical (ISTUN), University of Navarra, Pamplona, Spain"},{"name":"Department of Microbiology and Parasitology, University of Navarra, IdiSNA, Navarra Institute for Health Research, Pamplona, Spain"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Andr\u00e9s","family":"Vacas","sequence":"additional","affiliation":[{"name":"Instituto de Salud Tropical (ISTUN), University of Navarra, Pamplona, Spain"},{"name":"Department of Microbiology and Parasitology, University of Navarra, IdiSNA, Navarra Institute for Health Research, Pamplona, Spain"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Elena","family":"Iba\u00f1ez","sequence":"additional","affiliation":[{"name":"Center for Applied Medical Research (CIMA), University of Navarra, Pamplona, Spain"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Esther","family":"Moreno","sequence":"additional","affiliation":[{"name":"Instituto de Salud Tropical (ISTUN), University of Navarra, Pamplona, 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