{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,20]],"date-time":"2026-02-20T01:39:06Z","timestamp":1771551546108,"version":"3.50.1"},"reference-count":22,"publisher":"Wiley","issue":"4","license":[{"start":{"date-parts":[[2013,3,21]],"date-time":"2013-03-21T00:00:00Z","timestamp":1363824000000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Chem Biol Drug Des"],"published-print":{"date-parts":[[2013,4]]},"abstract":"<jats:p>A small series of thiazolidine\u20102,4\u2010dione and barbituric acid derivatives <jats:bold>1\u20134<\/jats:bold> was prepared using a short synthetic route, and all compounds were characterized by elemental analysis, mass spectrometry, and <jats:styled-content style=\"fixed-case\">NMR<\/jats:styled-content> (<jats:sup>1<\/jats:sup><jats:styled-content style=\"fixed-case\"><jats:roman>H<\/jats:roman><\/jats:styled-content>, <jats:sup>13<\/jats:sup><jats:styled-content style=\"fixed-case\"><jats:roman>C<\/jats:roman><\/jats:styled-content>) spectroscopy. Their <jats:italic>in vitro<\/jats:italic> relative expression of peroxisome proliferator\u2010activated receptor &amp;agr1; and peroxisome proliferator\u2010activated receptor &amp;ggr1; was evaluated. Compound <jats:bold>1<\/jats:bold> showed an increase in the m<jats:styled-content style=\"fixed-case\">RNA<\/jats:styled-content> expression of both peroxisome proliferator\u2010activated receptor isoforms, as well as the <jats:styled-content style=\"fixed-case\">GLUT<\/jats:styled-content>\u20104 levels. The antidiabetic activity of compound <jats:bold>1<\/jats:bold> was determined at 50\u00a0mg\/kg single dose using a non\u2010insulin\u2010dependent diabetes mellitus rat model. The results indicated a significant decrease in plasma glucose levels. Additionally, we performed a molecular docking of compound <jats:bold>1<\/jats:bold> into the ligand binding pocket of peroxisome proliferator\u2010activated receptor &amp;agr1; and peroxisome proliferator\u2010activated receptor &amp;ggr1;. In these binding models, compound <jats:bold>1<\/jats:bold> may bind into the active site of both isoforms showing important short contacts with the peroxisome proliferator\u2010activated receptor &amp;ggr1; residues: <jats:styled-content style=\"fixed-case\">T<\/jats:styled-content>yr 473, <jats:styled-content style=\"fixed-case\">H<\/jats:styled-content>is 449, <jats:styled-content style=\"fixed-case\">S<\/jats:styled-content>er 289, <jats:styled-content style=\"fixed-case\">H<\/jats:styled-content>is 323; and peroxisome proliferator\u2010activated receptor \u03b1 residues: <jats:styled-content style=\"fixed-case\">T<\/jats:styled-content>yr 464, <jats:styled-content style=\"fixed-case\">H<\/jats:styled-content>is 440, <jats:styled-content style=\"fixed-case\">S<\/jats:styled-content>er 280 and <jats:styled-content style=\"fixed-case\">T<\/jats:styled-content>yr 314.<\/jats:p>","DOI":"10.1111\/cbdd.12102","type":"journal-article","created":{"date-parts":[[2013,1,5]],"date-time":"2013-01-05T10:36:53Z","timestamp":1357382213000},"page":"474-483","source":"Crossref","is-referenced-by-count":57,"title":["Discovery of Thiazolidine\u20102,4\u2010Dione\/Biphenylcarbonitrile Hybrid as Dual <scp>PPAR<\/scp> \u03b1\/\u03b3 Modulator with Antidiabetic Effect: <i>In vitro, In Silico<\/i> and <i>In Vivo<\/i> Approaches"],"prefix":"10.1111","volume":"81","author":[{"given":"Sergio","family":"Hidalgo\u2010Figueroa","sequence":"first","affiliation":[{"name":"Facultad de Farmacia Universidad Aut\u00f3noma del Estado de Morelos Av. Universidad 1001 Chamilpa Cuernavaca Mor. 62209 M\u00e9xico"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Juan J.","family":"Ram\u00edrez\u2010Espinosa","sequence":"additional","affiliation":[{"name":"Facultad de Farmacia Universidad Aut\u00f3noma del Estado de Morelos Av. Universidad 1001 Chamilpa Cuernavaca Mor. 62209 M\u00e9xico"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Samuel","family":"Estrada\u2010Soto","sequence":"additional","affiliation":[{"name":"Facultad de Farmacia Universidad Aut\u00f3noma del Estado de Morelos Av. Universidad 1001 Chamilpa Cuernavaca Mor. 62209 M\u00e9xico"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Julio C.","family":"Almanza\u2010P\u00e9rez","sequence":"additional","affiliation":[{"name":"Laboratorio de Farmacolog\u00eda Depto. Ciencias de la Salud, D.C.B.S. Universidad Aut\u00f3noma Metropolitana\u2010Iztapalapa Apdo.\u2010Postal 55\u2013535 CP 09340 M\u00e9xico D.F. M\u00e9xico"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rub\u00e9n","family":"Rom\u00e1n\u2010Ramos","sequence":"additional","affiliation":[{"name":"Laboratorio de Farmacolog\u00eda Depto. Ciencias de la Salud, D.C.B.S. Universidad Aut\u00f3noma Metropolitana\u2010Iztapalapa Apdo.\u2010Postal 55\u2013535 CP 09340 M\u00e9xico D.F. M\u00e9xico"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Francisco J.","family":"Alarc\u00f3n\u2010Aguilar","sequence":"additional","affiliation":[{"name":"Laboratorio de Farmacolog\u00eda Depto. Ciencias de la Salud, D.C.B.S. Universidad Aut\u00f3noma Metropolitana\u2010Iztapalapa Apdo.\u2010Postal 55\u2013535 CP 09340 M\u00e9xico D.F. M\u00e9xico"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jes\u00fas V.","family":"Hern\u00e1ndez\u2010Rosado","sequence":"additional","affiliation":[{"name":"Posgrado en Biolog\u00eda Experimental, D.C.B.S. 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