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首页> 外文期刊>Archiv der Pharmazie >Synthesis and evaluation of 1,ω-bis(1,2,3,5-thiatriazol-5-yl)alkanes as in vitro and in vivo α-amylase and lipase inhibitors
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Synthesis and evaluation of 1,ω-bis(1,2,3,5-thiatriazol-5-yl)alkanes as in vitro and in vivo α-amylase and lipase inhibitors

机译：1，ω-双（1,2,3,5-噻三唑-5-基）烷烃的合成和评价作为体内和体外α-淀粉酶和脂肪酶抑制剂

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Thionyl chloride reacts with 1,ω-bis-(1-tosylamidrazone)alkanes 1 to give a series of 1,ω-bis-(4-alkyl-2-tosyl-1,2,3,5-thiatriazol-5-yl)alkanes 2. All the newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, elemental analysis, and ESI-MS spectral data. All the new compounds were screened for their inhibitory effect on key enzymes related to diabetes and obesity, such as α-amylase and lipase. In vitro and in vivo studies revealed that these thiatriazole derivatives exert an inhibitory action against these key enzymes. Moreover the administration of these compounds to surviving diabetic rats induced a significant decrease in plasma glucose level. Additively 2d significantly protected the liver-kidney functions and modulated lipid metabolism, which were evidenced by the decrease in aspartate transaminase (AST), alanine transaminase (ALT), and gamma-glutamyl transpeptidase (GGT) activities and creatinine, urea albumin, LDL-cholesterol and triglycerides levels as well as an increase in the HDL-cholesterol level in surviving diabetic rats. Overall, the findings of the current study indicate that 2d exhibits attractive properties and can, therefore, be considered for future application in the development of anti-diabetic and hypolipidemic drugs. A newly synthesized series of 1,ω-bis-(4-alkyl-2-tosyl-1,2,3,5- thiatriazol-5-yl)alkanes 2 were screened for their inhibitory effect on key enzymes related to diabetes and obesity, such as α-amylase and lipase. The administration of these compounds to surviving diabetic rats induced a significant decrease in plasma glucose levels. 2d significantly protected the liver-kidney functions and modulated lipid metabolism. Overall, compound 2d exhibited attractive properties, which make it interesting for future application in the development of anti-diabetic and hypolipidemic drugs.
机译：亚硫酰氯与1，ω-双-（1-甲苯磺酰ami）烷烃1反应生成一系列1，ω-双-（4-烷基-2-甲苯磺酰基-1,2,3,5-噻三唑-5-基烷烃2.所有新合成的化合物均经过IR，1H NMR，13C NMR，元素分析和ESI-MS光谱数据表征。筛选了所有新化合物对与糖尿病和肥胖相关的关键酶（如α-淀粉酶和脂肪酶）的抑制作用。体外和体内研究表明，这些噻三唑衍生物对这些关键酶具有抑制作用。而且，向存活的糖尿病大鼠施用这些化合物引起血浆葡萄糖水平的显着降低。加性2d可显着保护肝肾功能并调节脂质代谢，这通过降低天冬氨酸转氨酶（AST），丙氨酸转氨酶（ALT）和γ-谷氨酰转肽酶（GGT）活性以及肌酐，尿素白蛋白，LDL-存活的糖尿病大鼠体内的胆固醇和甘油三酸酯水平以及HDL-胆固醇水平升高。总体而言，当前研究的结果表明2d具有吸引人的特性，因此可以考虑将其用于抗糖尿病和降血脂药物的开发。筛选了一系列新合成的1，ω-双-（4-烷基-2-甲苯磺酰基-1,2,3,5-噻三唑-5-基）烷烃2对与糖尿病和肥胖相关的关键酶的抑制作用，例如α-淀粉酶和脂肪酶。向存活的糖尿病大鼠施用这些化合物导致血浆葡萄糖水平显着降低。 2d可显着保护肝肾功能并调节脂质代谢。总体而言，化合物2d表现出诱人的性能，这使其在抗糖尿病药和降血脂药的开发中具有广阔的应用前景。

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