title: Synthesis and Evaluation of 1-Substituted-Biguanide Derivatives as Anti-Diabetic Agents for Type II Diabetes Insulin Resistant.
abstract: New 1-substituted-biguanide derivatives 1-3 were synthesized by the reaction of 2,4-dimethoxyaniline, hydrazine and methylhydrazine with dicyandiamide in diluted hydrochloric acid. The resulting biguanide salts were fully characterized by spectroscopic methods. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives (200 mg/kg/day) for 2 weeks significantly decreased the elevated blood glucose level. Oral administration of biguanide derivative 2 significantly decreased the level of total cholesterol. While, the triglycerides level was little decreased following administration of biguanide 1 as compared to hyperglycemic rats. Additionally, anti-diabetic properties towards liver function enzyme activities (AST and ALT) and kidney functions (urea and critinine) as well as histopathological studies relative to metformin hydrochloride were investigated and discussed.
authors.affiliation: Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.
authors.forename: S Y
authors.initials: SY
authors.lastname: Abbas
authors.affiliation: Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.
authors.forename: W M
authors.initials: WM
authors.lastname: Basyouni
authors.affiliation: Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt.
authors.forename: K A M
authors.initials: KA
authors.lastname: El-Bayouki
authors.affiliation: Pharmacology Department, National Research Centre, Cairo, Egypt.
authors.forename: R F
authors.initials: RF
authors.lastname: Abdel-Rahman
mesh_terms: D000410:Alanine Transaminase / Q000097:blood; D000818:Animals; D001219:Aspartate Aminotransferases / Q000097:blood; D001645:Biguanides / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D001786:Blood Glucose; D002784:Cholesterol / Q000097:blood; D003404:Creatinine / Q000652:urine; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy* / Q000473:pathology; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000627:therapeutic use; D007333:Insulin Resistance; D008099:Liver / Q000473:pathology; D008297:Male; D008687:Metformin / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D014280:Triglycerides / Q000097:blood; D014508:Urea / Q000652:urine
chemical_list: D001645:Biguanides; D001786:Blood Glucose; D007004:Hypoglycemic Agents; D014280:Triglycerides; D014508:Urea; D008687:Metformin; D002784:Cholesterol; D003404:Creatinine; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase