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Synthesis and Biological Evaluation of Some Novel Coumarin and Guanidine Derivatives by Oral Glucose Tolerance Test

Vahan G. Prajapati and Dr. Dhrubo Jyoti Sen

Objective: The major drawback of current treatment of diabetes is challenging due to resistance to antidiabetic agents their side effects. Chromenes occurs naturally in plants and plays role of anticoagulant activity. Guanidine plays role of antidiabetic activity. 2H-chromenes are the heterocyclic compounds with considerable therapeutic and pharmacological properties. Guanidine is compounds with considerable therapeutic and pharmacological properties. In this view, it has been planned to combine both guanidine and coumarin derivatives. Biological activity for antidiabetic activity has been performed for guanidine derivatives.

Experimental and Computational work done: 2H-chromene was synthesized by Pechmann condensation of resorcinol, ethyl acetoacetate and sulphuric acid. Then coumarin was combined with guanidine. This combined compound was substituted by different substituted benzaldehyde and in other series by oxidation, chlorination and Schotten Baumann reaction. The purity of the compounds was checked by TLC monitoring and all the synthesized compounds were characterized by UV, IR, Mass and some of by 1H-NMR spectroscopy. The antidiabetic activities of synthesized compounds were tested by oral glucose tolerance test (OGTT).

Results and discussion: In antidiabetic activity, compounds 9-b have shown highest antidiabetic activity while compounds 9-a and 11-a have shown also antidiabetic activity against metformin as standard.

Conclusion: Evaluation of antidiabetic revealed that compounds with substituted benzaldehyde at the 4-position of the phenyl ring of 2H-chromenes and at oxidation, chlorination and Schotten Baumann reaction of synthesized intermediate i.e., 9-a is most active antidiabetic agent.