Abbas Samir Y, Basyouni Wahid M, El-Bayouk Khairy A M, Tohamy Wael M, Aly Hanan F, Arafa Azza, Soliman Mahmoud S
Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.
Therapeutic Chemistry Department, National Research Centre, Cairo, Egypt.
Drug Res (Stuttg). 2017 Oct;67(10):557-563. doi: 10.1055/s-0043-102692. Epub 2017 Jun 26.
New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level. Additionally, anti-diabetic properties towards liver function enzyme activities (AST, ALT and ALP), lipids profiles (TC, TG and TL), lipid peroxide and nitrous oxide as well as histopathological studies relative to metformin hydrochloride were investigated and discussed.
通过在酸性介质中使苯并[1,3 - d]二氧杂环戊烯 - 5 - 胺、苯肼、N,N - 二甲基肼甲酰胺、苯甲酰肼和2 - 苯基乙酰肼与双氰胺反应，合成了新的1 - 取代 - 盐酸双胍盐。用光谱工具对所得双胍盐的结构进行了表征。用标准二甲双胍药物对合成的化合物进行抗糖尿病活性筛选。用合成的双胍衍生物口服治疗高血糖大鼠可显著降低升高的血糖水平。此外，还研究并讨论了相对于盐酸二甲双胍，其对肝功能酶活性（AST、ALT和ALP）、血脂谱（TC、TG和TL）、脂质过氧化物和一氧化氮的抗糖尿病特性以及组织病理学研究。
