新型磺酰基双胍和磺酰脲衍生物的合成及高血糖、生化和组织病理学评价作为有效的抗糖尿病药物。
Synthesis and hyperglycemic, biochemical and histopathological evaluation of novel sulfonylbiguanide and sulfonylurea derivatives as potent anti-diabetic agents.
机构信息
Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.
Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.
出版信息
Bioorg Chem. 2021 Dec;117:105418. doi: 10.1016/j.bioorg.2021.105418. Epub 2021 Oct 12.
New sulfonylbiguanide hydrochloride salts and sulfonylurea derivatives containing two sulfonyl groups were synthesized through the reaction of arylsulfonohydrazides with cyanoguanidine and p-tolylsulfonylisocyanate, respectively. Oral treatment of hyperglycemic rats with the synthesized sulfonylbiguanide derivatives 2 and sulfonylurea derivatives 3 revealed that sulfonylurea derivatives 3a and 3c possessed significant decrease of the elevated glucose in compression with the anti-diabetic standard drugs. Effects of the synthesized sulfonylurea derivatives 3a and 3c on the diabetic properties towards α-amylase, liver function enzyme levels (AST, ALT, ALP, TB and γ-GT), kidney functions (urea and creatinine), lipids profiles (TG, TL, TC and HDL-C) were studied. Also, the effect of sulfonylurea derivatives 3a and 3c as antioxidants (reduced glutathione and lipid peroxide) was evaluated. Histopathological examination of hepatic and pancreatic tissues was investigated. The obtained results suggested that the most potent sulfonylurea derivatives 3a and 3c might be possible used as novel diabetic inhibitor agents.
通过芳基磺酰腙与氰胍和对甲苯磺酰异氰酸酯的反应，分别合成了含有两个磺酰基的新型磺酰双胍盐酸盐盐和磺酰脲衍生物。将合成的磺酰双胍衍生物 2 和磺酰脲衍生物 3 对高血糖大鼠进行口服治疗，结果表明磺酰脲衍生物 3a 和 3c 具有显著降低升高的葡萄糖的作用，与抗糖尿病标准药物相当。研究了合成的磺酰脲衍生物 3a 和 3c 对α-淀粉酶、肝功能酶水平（AST、ALT、ALP、TB 和 γ-GT）、肾功能（尿素和肌酐）、脂质谱（TG、TL、TC 和 HDL-C）的糖尿病特性的影响。还评估了磺酰脲衍生物 3a 和 3c 作为抗氧化剂（还原型谷胱甘肽和脂质过氧化物）的效果。研究了肝和胰腺组织的组织病理学检查。结果表明，最有效的磺酰脲衍生物 3a 和 3c 可能可用作新型糖尿病抑制剂。
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