Chemistry and hypoglycemic activity of benzimidoylpyrazoles

Abstract
A series of benzimidoylpyrazoles was synthesized and evaluated as hypoglycemic agents. Methyl 1-(N-cyclohexylbenzimidoyl)-5-methyl-3-pyrazolecarboxylate and methyl 1-[N-(4-methoxyphenyl)benzimidoyl]-5-methyl-3-pyrazolecarboxylate are 2 of the more interesting compounds. A comparison of these benzimidoylpyrazoles with classical standards (tolazamide, phenformin and buformin) in rats show that these compounds seem to combine in 2 molecule some of the biological activities of the .beta.-cytotrophic sulfonylureas and some of the activities of the biguanides. A synthetic scheme for the preparation of the benzimidoylpyrazoles and a preliminary structure-activity relationship are presented.

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