{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,13]],"date-time":"2026-02-13T04:45:32Z","timestamp":1770957932737,"version":"3.50.1"},"reference-count":0,"publisher":"Bentham Science Publishers Ltd.","issue":"27","content-domain":{"domain":["eurekaselect.com"],"crossmark-restriction":true},"short-container-title":["CTMC"],"published-print":{"date-parts":[[2019,1,31]]},"abstract":"<jats:sec>\n<jats:title\/>\n<jats:p>Diabetes mellitus type 2 (DMT2) is a metabolic disease characterized by a chronic increase in\nglycemia that promotes several long-term complications and high mortality. Some enzymes involved in\nglycaemic control, such as \u03b1 -(1,4)-glucosidase, have now been established as novel pharmacological\ntargets. Coumarins have shown benefits in attenuating signs and complications of DMT2, including inhibition\nof this enzyme. In this work, new synthetic coumarins (bearing different amide and aryl substituents)\nwere studied in vitro as inhibitors of \u03b1-(1,4)-glucosidase. Among them, five molecules proved to\nbe excellent \u03b1-(1,4)-glucosidase inhibitors, being compound 7 (IC50 = 2.19 \u00b5M) about 200 times more\npotent than acarbose, a drug currently used for the treatment of DMT2. In addition, most of the coumarins\npresented uncompetitive inhibition for the \u03b1-(1,4)-glucosidase. Molecular docking studies revealed\nthat coumarins bind to the active site of the enzyme in a more external area comparing to the substrate,\nwithout interfering with it, and displaying aromatic and hydrophobic interactions, as well as some hydrogen\nbonds. According to the results, aromatic interactions with two phenylalanine residues, 157 and\n177, were the most common among the studied coumarins. This study is a step forward for the understanding\nof coumarins as potential anti-diabetic compounds displaying \u03b1-(1,4)-glucosidase inhibition.<\/jats:p>\n<\/jats:sec>","DOI":"10.2174\/1568026619666181130113033","type":"journal-article","created":{"date-parts":[[2018,11,30]],"date-time":"2018-11-30T12:02:02Z","timestamp":1543579322000},"page":"2327-2337","update-policy":"https:\/\/doi.org\/10.2174\/bsp_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Targeting \u03b1 -(1,4)-Glucosidase in Diabetes Mellitus Type 2: The Role of New Synthetic Coumarins as Potent Inhibitors"],"prefix":"10.2174","volume":"18","author":[{"given":"Catalina","family":"Figueroa-Benavides","sequence":"first","affiliation":[{"name":"Departamento de Quimica Farmacologica y Toxicologica, Laboratorio de Productos Naturales, Facultad de Ciencias Quimicas y Farmaceuticas, Universidad de Chile, Santos Dumont 964, Independencia, Santiago, Chile"}]},{"given":"Maria Jo\u00e3o","family":"Matos","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain"}]},{"given":"Montserrat","family":"Pe\u00f1aloza-Amion","sequence":"additional","affiliation":[{"name":"Inorganic and Analytical Chemistry Department, Laboratory, Department, Molecular Graphic Unit, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Sergio Livingstone 1007, Independencia, Santiago, Chile"}]},{"given":"Rub\u00e9n","family":"Veas","sequence":"additional","affiliation":[{"name":"Departamento de Quimica Farmacologica y Toxicologica, Laboratorio de Productos Naturales, Facultad de Ciencias Quimicas y Farmaceuticas, Universidad de Chile, Santos Dumont 964, Independencia, Santiago, Chile"}]},{"given":"Gabriela","family":"Valenzuela-Barra","sequence":"additional","affiliation":[{"name":"Departamento de Quimica Farmacologica y Toxicologica, Laboratorio de Productos Naturales, Facultad de Ciencias Quimicas y Farmaceuticas, Universidad de Chile, Santos Dumont 964, Independencia, Santiago, Chile"}]},{"given":"Gerald","family":"Zapata","sequence":"additional","affiliation":[{"name":"Inorganic and Analytical Chemistry Department, Laboratory, Department, Molecular Graphic Unit, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Sergio Livingstone 1007, Independencia, Santiago, Chile"}]},{"given":"Giovanna","family":"Delogu","sequence":"additional","affiliation":[{"name":"Department of Life and Environmental Sciences, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy"}]},{"given":"Eugenio","family":"Uriarte","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain"}]},{"given":"Lourdes","family":"Santana","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain"}]},{"given":"Claudio","family":"Olea-Azar","sequence":"additional","affiliation":[{"name":"Free Radical and Antioxidants Laboratory, Inorganic and Analytical Department, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Sergio Livingstone 1007, Independencia, Santiago, Chile"}]},{"given":"Carla","family":"Delporte","sequence":"additional","affiliation":[{"name":"Departamento de Quimica Farmacologica y Toxicologica, Laboratorio de Productos Naturales, Facultad de Ciencias Quimicas y Farmaceuticas, Universidad de Chile, Santos Dumont 964, Independencia, Santiago, Chile"}]}],"member":"965","container-title":["Current Topics in Medicinal 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