New Biguanides as Anti-Diabetic Agents Part I: Synthesis and Evaluation of 1-Substituted Biguanide Derivatives as Anti-Diabetic Agents of Type II Diabetes Insulin Resistant

Drug Res (Stuttg). 2017 Oct;67(10):557-563. doi: 10.1055/s-0043-102692. Epub 2017 Jun 26.

Abstract

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.

MeSH terms

  • Animals
  • Biguanides / chemical synthesis*
  • Biguanides / pharmacology*
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetes Mellitus, Type 2 / blood
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / pharmacology*
  • Insulin Resistance
  • Lipids / blood*
  • Liver / drug effects*
  • Metformin / pharmacology*
  • Metformin / therapeutic use*
  • Nitrous Oxide / chemistry*
  • Rats

Substances

  • Biguanides
  • Hypoglycemic Agents
  • Lipids
  • Metformin
  • Nitrous Oxide