دورية أكاديمية
Synthesis, Computational Study, and In Vitro α-Glucosidase Inhibitory Action of 1,3,4-Thiadiazole Derivatives of 3-Aminopyridin-2(1 H)-ones.
العنوان: | Synthesis, Computational Study, and In Vitro α-Glucosidase Inhibitory Action of 1,3,4-Thiadiazole Derivatives of 3-Aminopyridin-2(1 H)-ones. |
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المؤلفون: | Shulgau, Zarina, Palamarchuk, Irina V., Sergazy, Shynggys, Urazbayeva, Assel, Ramankulov, Yerlan, Kulakov, Ivan V. |
المصدر: | Pharmaceuticals (14248247); Mar2024, Vol. 17 Issue 3, p377, 15p |
مصطلحات موضوعية: | THIADIAZOLES, BENZOIC acid, BENZOATES, PHTHALIC acid, MOLECULAR docking, ACID derivatives |
مستخلص: | This article reports on the synthesis of nine promising new 1,3,4-thiadiazole derivatives based on 3-aminopyridones, containing various acidic linkers. The synthesis was carried out by cyclizing the corresponding thiohydrazides 4a–c and anhydrides of glutaric, maleic, and phthalic acids upon heating in acetic acid solution. The conducted bio-screening of the synthesized new 1,3,4-thiadiazole derivatives containing different acidic linkers (butanoic, acrylic, and benzoic acids) showed that they have significant inhibitory activity against α-glucosidase (up to 95.0%), which is 1.9 times higher than the value for the reference drug acarbose (49.5%). Moreover, one of the 1,3,4-thiadiazole derivatives with a benzoic acid linker—2-(5-((6-Methyl-2-oxo-4-(thiophen-2-yl)-1,2-dihydropyridin-3-yl)carbamoyl)-1,3,4-thiadiazol-2-yl)benzoic acid (9′b)—showed an IC |
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قاعدة البيانات: | Complementary Index |
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