<?xml version="1.0" encoding="ISO-8859-1"?><article xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink" xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance">
<front>
<journal-meta>
<journal-id>0120-2804</journal-id>
<journal-title><![CDATA[Revista Colombiana de Química]]></journal-title>
<abbrev-journal-title><![CDATA[Rev.Colomb.Quim.]]></abbrev-journal-title>
<issn>0120-2804</issn>
<publisher>
<publisher-name><![CDATA[Departamento de Química,  Universidad Nacional de Colombia.]]></publisher-name>
</publisher>
</journal-meta>
<article-meta>
<article-id>S0120-28042022000300003</article-id>
<article-id pub-id-type="doi">10.15446/rev.colomb.quim.v51n3.105911</article-id>
<title-group>
<article-title xml:lang="en"><![CDATA[Design, synthesis, in silico studies, and antidiabetic activity of several sulfanilamide incorporated 2,3-disubstitut-ed thiazolidin-4-ones]]></article-title>
<article-title xml:lang="es"><![CDATA[Diseño, síntesis, estudios in silico y actividad antidiabética de algunas sulfanilamidas 2,3-disustituidas tiazolidi-na-4-onas incorporadas]]></article-title>
<article-title xml:lang="pt"><![CDATA[Concepção, síntese, em estudos de silico e atividade antidiabética de poucas sulfanilamidas incorporado 2,3-disubstituído thiazolidi-na-4-ones]]></article-title>
</title-group>
<contrib-group>
<contrib contrib-type="author">
<name>
<surname><![CDATA[Deshpande]]></surname>
<given-names><![CDATA[Shreenivas R.]]></given-names>
</name>
<xref ref-type="aff" rid="Aff"/>
</contrib>
<contrib contrib-type="author">
<name>
<surname><![CDATA[Wader]]></surname>
<given-names><![CDATA[Mallikarjun S.]]></given-names>
</name>
<xref ref-type="aff" rid="Aff"/>
</contrib>
<contrib contrib-type="author">
<name>
<surname><![CDATA[Malagi]]></surname>
<given-names><![CDATA[Prasad V.]]></given-names>
</name>
<xref ref-type="aff" rid="Aff"/>
</contrib>
<contrib contrib-type="author">
<name>
<surname><![CDATA[Jalihal]]></surname>
<given-names><![CDATA[Prabhu C.]]></given-names>
</name>
<xref ref-type="aff" rid="Aff"/>
</contrib>
</contrib-group>
<aff id="Af1">
<institution><![CDATA[,Hanagal Shri Kumareshwar College of Pharmacy Department of Medicinal and Pharmaceutical Chemistry ]]></institution>
<addr-line><![CDATA[Karnataka ]]></addr-line>
<country>India</country>
</aff>
<pub-date pub-type="pub">
<day>00</day>
<month>12</month>
<year>2022</year>
</pub-date>
<pub-date pub-type="epub">
<day>00</day>
<month>12</month>
<year>2022</year>
</pub-date>
<volume>51</volume>
<numero>3</numero>
<fpage>3</fpage>
<lpage>13</lpage>
<copyright-statement/>
<copyright-year/>
<self-uri xlink:href="http://www.scielo.org.co/scielo.php?script=sci_arttext&amp;pid=S0120-28042022000300003&amp;lng=en&amp;nrm=iso"></self-uri><self-uri xlink:href="http://www.scielo.org.co/scielo.php?script=sci_abstract&amp;pid=S0120-28042022000300003&amp;lng=en&amp;nrm=iso"></self-uri><self-uri xlink:href="http://www.scielo.org.co/scielo.php?script=sci_pdf&amp;pid=S0120-28042022000300003&amp;lng=en&amp;nrm=iso"></self-uri><abstract abstract-type="short" xml:lang="en"><p><![CDATA[Abstract A panel of 2,3-disubstituted thiazolidin-4-ones 4a-n was synthesised from Schiff bases 3a-n derived from sulfanilamide, by reaction with thioglycolic acid. The compounds were characterised by means of IR, NMR, and Mass spectral data. Compounds 4a-n were screened for DPPH scavenging assay and compounds 4e, 4h, 4i, and 4n exhibited moderate activity. Compounds 4e, 4h, and 4i were tested at 200 mg/kg and 4e at 50 mg/kg b.w. orally for antidiabetic activity in fructose induced diabetic rats. They exhibited significant antidiabetic activity compared to the control group. Pioglitazone was used as a standard drug. The tested compounds exhibited better and ignificant serum cholesterol lowering activity when compared with the control and standard groups. They also reduced the triglyceride level after the 21st day; however, it was insignificant when compared to the control group. Compound 4n displayed the highest binding energy when docked with PPAR-&#947; followed by compounds 4e, 4h, and 4i when compared to pioglitazone. The physicochemical, drug likeness and ADME properties of the title compounds were found to be satisfactory.]]></p></abstract>
<abstract abstract-type="short" xml:lang="es"><p><![CDATA[Resumen Se sintetizó un panel de tiazolidinas-4-onas 2,3-disustituidas 4a-n a partir de las bases de Schiff 3a-n derivadas de la sulfanilamida por reacción con ácido tioglicólico. Los compuestos se caracterizaron por IR, RMN y datos espectrales de masa. Los compuestos 4a-n se analizaron para DPPH y los compuestos 4e, 4h, 4i y 4n mostraron una actividad moderada. Los compuestos 4e, 4h y 4i se probaron a 200 mg/kg y 4e a 50 mg/kg b.w. oralmente para la actividad antidiabética en ratas diabéticas, inducida por fructosa. Los compuestos mostraron una actividad antidiabética muy significativa en comparación con el grupo control. La pioglitazona se utilizó como fármaco estándar. Los compuestos ensayados mostraron una mejor y significativa actividad reductora del colesterol sérico en comparación con los grupos control y estándar. Estos compuestos también redujeron el nivel de triglicéridos después del 21° día, aunque fue insignificante en comparación con el grupo control. El compuesto 4n mostró la mayor afinidad de unión cuando se acopló a PPAR-&#947;, seguido de 4e, 4h y 4i en comparación con la pioglitazona. Las propiedades fisicoquímicas, la similitud con el fármaco y las propiedades ADME de los compuestos fueron satisfactorias, lo que los convierte en útiles agentes antidiabéticos.]]></p></abstract>
<abstract abstract-type="short" xml:lang="pt"><p><![CDATA[Resumo Um painel de 2,3-disubstituído thiazolidina-4-ones 4a-n foram sintetizados a partir de bases Schiff 3a-n derivado da sulfanilamida por reacção com ácido tioglicólico. Os compostos eram caracterizado por IR, NMR e dados espectrais de massa. Os compostos 4a-n foram rastreados para O ensaio DPPH de limpeza radical e os compostos 4e, 4h, 4i e 4n exibiram actividade moderada. Os compostos 4e, 4h e 4i foram testados a 200 mg/kg e 4e a 50 mg/kg de peso corporal por via oral para antidiabéticos. actividade em ratos diabéticos induzidos por frutose. Exibiram uma actividade antidiabética altamente significativa actividade em comparação com o controlo. A pioglitazona foi utilizada como droga padrão. Os compostos testados exibiu uma melhor e significativa actividade de redução do colesterol sérico quando comparado comde triglicéridos após o 21° dia; no entanto, foi insignificante quando comparado com o controlo. O composto 4n mostrou a maior afinidade de ligação quando acoplado com PPAR-&#947; seguido de 4e, 4h, 4i quando comparado com pioglitazona. O propriedades físico-químicas, de semelhança com drogas e ADME dos compostos do título de propriedade também foram encontrados paraser satisfatórios, tornando-os agentes antidiabéticos úteis.]]></p></abstract>
<kwd-group>
<kwd lng="en"><![CDATA[Schiff bases]]></kwd>
<kwd lng="en"><![CDATA[DPPH]]></kwd>
<kwd lng="en"><![CDATA[antioxidant]]></kwd>
<kwd lng="en"><![CDATA[serum glucose]]></kwd>
<kwd lng="en"><![CDATA[total serum cholesterol]]></kwd>
<kwd lng="en"><![CDATA[serum triglycerides]]></kwd>
<kwd lng="en"><![CDATA[PPAR-y]]></kwd>
<kwd lng="en"><![CDATA[ADME]]></kwd>
<kwd lng="en"><![CDATA[Drug Likeness]]></kwd>
<kwd lng="es"><![CDATA[Bases de Schiff]]></kwd>
<kwd lng="es"><![CDATA[DPPH]]></kwd>
<kwd lng="es"><![CDATA[antioxidante]]></kwd>
<kwd lng="es"><![CDATA[glucosa sérica]]></kwd>
<kwd lng="es"><![CDATA[colesterol total sérico]]></kwd>
<kwd lng="es"><![CDATA[triglicéridos séricos triglicéridos séricos]]></kwd>
<kwd lng="es"><![CDATA[PPAR-y]]></kwd>
<kwd lng="es"><![CDATA[ADME]]></kwd>
<kwd lng="es"><![CDATA[similitud de fármacos]]></kwd>
<kwd lng="pt"><![CDATA[bases Schiff]]></kwd>
<kwd lng="pt"><![CDATA[DPPH]]></kwd>
<kwd lng="pt"><![CDATA[antioxidante]]></kwd>
<kwd lng="pt"><![CDATA[glucose sérica]]></kwd>
<kwd lng="pt"><![CDATA[colesterol total sérico]]></kwd>
<kwd lng="pt"><![CDATA[soro triglicéridos]]></kwd>
<kwd lng="pt"><![CDATA[PPAR-y]]></kwd>
<kwd lng="pt"><![CDATA[ADME]]></kwd>
<kwd lng="pt"><![CDATA[Probabilidade de drogas]]></kwd>
</kwd-group>
</article-meta>
</front><back>
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