{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,5]],"date-time":"2026-03-05T07:46:24Z","timestamp":1772696784742,"version":"3.50.1"},"reference-count":30,"publisher":"MDPI AG","issue":"2","license":[{"start":{"date-parts":[[2017,1,30]],"date-time":"2017-01-30T00:00:00Z","timestamp":1485734400000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Leishmaniases are a group of neglected tropical diseases (NTDs) caused by protozoan parasites from &gt;20 Leishmania species. Visceral leishmaniasis (VL), also known as kala\u2010aza, is the most severe form of leishmaniasis, usually fatal in the absence of treatment in 95% of cases. The Morita\u2010Baylis\u2010Hillman adducts (MBHAs) are being explored as drug candidates against several diseases, one of them being leishmaniasis. We present here the design, synthesis and in vitro screening against Leishmania donovani of sixteen new molecular hybrids from analgesic\/antiinflammatory tetrahydropyrans derivatives and Morita\u02d7Baylis\u02d7Hillman adducts. First, acrylates were synthesized from analgesic\/anti\u2010inflammatory tetrahydropyrans using acrylic acid under TsOH as a catalyst (70\u201375% yields). After the 16 new MBHAs were prepared in moderate to good yields (60\u201395%) promoted by microwave irradiation or low temperature (0 \u00b0C) in protic and aprotic medium. The hybrids were evaluated in vitro on the promastigote stage of Leishmania donovani by determining their inhibitory concentrations 50% (IC50), 50% hemolysis  concentration (HC50), selectivity index (HC50\/IC50,), and comparing to Amphotericin B, chosen as the anti\u2010leishmanial reference drug. The hybrid which presents the bromine atom in its chemical structure presents high leishmanicide activity and the high selectivity index in red blood cells (SIrb &gt; 180.19), compared with the highly\u2010toxic reference drug (SIrb = 33.05), indicating that the bromine hybrid is a promising compound for further biological studies.<\/jats:p>","DOI":"10.3390\/molecules22020207","type":"journal-article","created":{"date-parts":[[2017,1,30]],"date-time":"2017-01-30T11:36:30Z","timestamp":1485776190000},"page":"207","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Synthesis of 16 New Hybrids from Tetrahydropyrans Derivatives and Morita\u02d7Baylis\u02d7Hillman Adducts: In Vitro Screening against Leishmania donovani"],"prefix":"10.3390","volume":"22","author":[{"given":"Suervy","family":"Sousa","sequence":"first","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Juliana","family":"Rocha","sequence":"additional","affiliation":[{"name":"Departamento de Biotecnologia, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tatjana","family":"Keesen","sequence":"additional","affiliation":[{"name":"Departamento de Biotecnologia, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Everton","family":"Silva","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Priscilla","family":"De Assis","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"},{"name":"Unidade Acad\u00eamica de Sa\u00fade, Centro de Educa\u00e7\u00e3o e Sa\u00fade, Universidade Federal de Campina Grande, Campus Cuit\u00e9, Cuit\u00e9, PB 58175\u2010000, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jo\u00e3o","family":"De Oliveira","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Saulo","family":"Capim","sequence":"additional","affiliation":[{"name":"Instituto Federal de Educa\u00e7\u00e3o, Ci\u00eancia e Tecnologia da Bahia, Campus Catu, Bar\u00e3o de Cama\u00e7ari, Catu, BA 48110\u2010000, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Francisco","family":"Xavier","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Bruno","family":"Marinho","sequence":"additional","affiliation":[{"name":"Programa de P\u00f3s\u2010Gradua\u00e7\u00e3o em Ci\u00eancias Fisiol\u00f3gicas and Laborat\u00f3rio de Farmacologia, Departamento Ci\u00eancias Fisiol\u00f3gicas, Instituto de Ci\u00eancias e Sa\u00fade, Universidade Federal Rural do Rio de Janeiro Serop\u00e9dica, RJ 23890\u2010000, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"F\u00e1bio","family":"Silva","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Claudio","family":"Lima\u2010Junior","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M\u00e1rio","family":"Vasconcellos","sequence":"additional","affiliation":[{"name":"Laborat\u00f3rio de S\u00edntese Org\u00e2nica Medicinal da Para\u00edba (LASOM\u2010PB), Departamento de Qu\u00edmica, Universidade Federal da Para\u00edba, Campus I, Jo\u00e3o Pessoa, PB 58059\u2010900, Brazil"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2017,1,30]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"179","DOI":"10.1093\/bmb\/ldp046","article-title":"Neglected tropical diseases","volume":"93","author":"Feasey","year":"2010","journal-title":"Br. 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Int."}],"container-title":["Molecules"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/www.mdpi.com\/1420-3049\/22\/2\/207\/pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,10,11]],"date-time":"2025-10-11T18:27:16Z","timestamp":1760207236000},"score":1,"resource":{"primary":{"URL":"https:\/\/www.mdpi.com\/1420-3049\/22\/2\/207"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2017,1,30]]},"references-count":30,"journal-issue":{"issue":"2","published-online":{"date-parts":[[2017,2]]}},"alternative-id":["molecules22020207"],"URL":"https:\/\/doi.org\/10.3390\/molecules22020207","relation":{},"ISSN":["1420-3049"],"issn-type":[{"value":"1420-3049","type":"electronic"}],"subject":[],"published":{"date-parts":[[2017,1,30]]}}}