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Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides |
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| Authors: | Moreno-Díaz Hermenegilda Villalobos-Molina Rafael Ortiz-Andrade Rolffy Díaz-Coutiño Daniel Medina-Franco Jose Luis Webster Scott P Binnie Margaret Estrada-Soto Samuel Ibarra-Barajas Maximiliano León-Rivera Ismael Navarrete-Vázquez Gabriel |
| Affiliation: | aFacultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico bUnidad de Biomedicina, FES Iztacala, Universidad Nacional Autónoma de México, Tlalnepantla, México 54090, Mexico cCentro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico dTorrey Pines Institute for Molecular Studies, Fort Pierce, FL 34946, USA eEndocrinology Unit, Centre for Cardiovascular Science, The Queen’s Medical Research Institute, University of Edinburgh, Edinburgh EH16 4TJ, UK |
| Abstract: | N-(6-Substituted-1,3-benzothiazol-2-yl)benzenesulfonamide derivatives 1–8 were synthesized and evaluated for their in vivo antidiabetic activity in a non-insulin-dependent diabetes mellitus rat model. Several compounds synthesized showed significant lowering of plasma glucose level in this model. As a possible mode of action, the compounds were in vitro evaluated as 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. The most active compounds (3 and 4) were docked into the crystal structure of 11β-HSD1. Docking results indicate potential hydrogen bond interactions with catalytic amino acid residues. |
| Keywords: | Diabetes Benzothiazole Streptozotocin–nicotinamide model |
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