Journal américain de l'administration avancée de médicaments Libre accès

Abstrait

Design, Synthesis and Oral Glucose Tolerance Screening of Some 5-substituted benzylidene-3 [2-(2-methyl-1H-benzimidazol-1-yl)-2-oxoethyl]-1,3 thiazolidine-2,4-dione Derivatives on Rats

Bhumika K. Prajapati and Dr. Dhrubo Jyoti Sen

Objective: As a part of research project, the knowledge gained by various researches has suggested that substituted benzimidazole which is the structural isosteres of nucleotides allow them to interact easily with the biopolymers, possess good pharmacological activity with lower toxicities. In recent years 2-methyl-1H-benzimidazole shows promising antihyperglycaemic activity. So, substituting or adding a new moiety to the parent lead compound thus by making gradual changes in the structure of compound resulting gradual change in physicochemical properties and biological activities of drug. All the synthesized compounds were characterized by UV, IR, Mass and some of by 1H-NMR spectroscopy & report of them supports the structures of compounds. Compounds 40a, 40b, 40e and 40h were found to be having significant glucose lowering effect as compared to control and standard. Other compounds like 40c, 40d, 40f and 40g were found to be lower active as compared to standard and other derivatives. Evaluation of antidiabetic activity revealed that compounds with acetylated benzimidazole having the thiazolidinedione moiety gives best biological activity having electron donating group at the 4th position of the phenyl ring i.e., 40a, 40b, 40e and 40h are most active with electron releasing functional groups are having good antidiabetic property. All the synthesized final compounds were screened for antidiabetic activity by Oral Glucose Tolerance Test (OGTT) method against standard reference drug pioglitazone.

Activity Scale: 40a>40b>40h>40e>40c>40d>40f>40g