Synthesis and Evaluation of 1-Substituted-Biguanide Derivatives as Anti-Diabetic Agents for Type II Diabetes Insulin Resistant.

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.

Synthesis and quarternization of 6-(substitutedamino)-purines with antitumor activity screening.

Reaction of 6-chloro-9-benzyl-8-(methylthio)purine 3 with primary amines afforded, the corresponding 6-(substitutedamino)purines 4a-g. The latter products when methylated with methyl iodide yielded smoothly N3-methyl purinium iodide salts 5a-f rather than the probable N1- and N7-derivatives. 9-Benzyl-3-methyl-6-(methylimino)-8-(methylthio)purine 8 was obtained upon treating the purinium iodide 5a with alkali. Most of the synthesized compounds were screened for their antitumor activity.

Synthesis of some new 3,5-pyrazolidinedione derivatives of expected biological activity.

4-Arylidene-1,2-diphenyl-3,5-pyrazolidinedione were synthetized. The alkyl and nitrile derivatives were also obtained. The structure of the synthesized compounds was elucidated by chemical and physical routes.