7 research outputs found

    NOx-emissions of a 40 MW pressurized fluidized bed combustor

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    Untersuchungen der Schadstoffemissionen einer Druckwirbelschichtfeuerung

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    SIGLEAvailable from TIB Hannover: DW 7449 / FIZ - Fachinformationszzentrum Karlsruhe / TIB - Technische InformationsbibliothekDEGerman

    Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and <i>in silico</i> insights

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    From Crossref journal articles via Jisc Publications RouterHistory: received 2023-05-24, revised 2023-06-23, accepted 2023-06-25, epub 2023-07-20, issued 2023-07-20, published 2023-07-20, ppub 2023-12-31Article version: VoRPublication status: PublishedFunder: King Saud University, Riyadh, Saudi Arabia; Grant(s): RSPD2023R74

    Development of new thiazolidine-2,4-dione hybrids as aldose reductase inhibitors endowed with antihyperglycaemic activity: design, synthesis, biological investigations, and <i>in silico</i> insights

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    This research study describes the development of new small molecules based on 2,4-thiazolidinedione (2,4-TZD) and their aldose reductase (AR) inhibitory activities. The synthesis of 17 new derivatives of 2,4-TZDs hybrids was feasible by incorporating two known bioactive scaffolds, benzothiazole heterocycle, and nitro phenacyl moiety. The most active hybrid (8b) was found to inhibit AR in a non-competitive manner (0.16 µM), as confirmed by kinetic studies and molecular docking simulations. Furthermore, the in vivo experiments demonstrated that compound 8b had a significant hypoglycaemic effect in mice with hyperglycaemia induced by streptozotocin. Fifty milligrams per kilogram dose of 8b produced a marked decrease in blood glucose concentration, and a lower dose of 5 mg/kg demonstrated a noticeable antihyperglycaemic effect. These outcomes suggested that compound 8b may be used as a promising therapeutic agent for the treatment of diabetic complications.</p
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