Five New Biguanides Synthesis And Their Effects On Blood Glucose Of Rats With Type â…¡ Diabetes

Biguanides are commonly used oral antihyperglycemic drugs in treating type II diabetes. Some of the biguanides, e.g., metformins (pheformin and buformin) are restricted in clinical application due to their untoward reaction of causing fatal lactic acidosis. Rather than stimulating insulin secretion, Metformin lowers blood glucose through inhibiting hepatic glyconeogenesis,increasing uptake and ultilization of glucose in peripheral targeting tissues and improving the sensitivity of tissue to insulin.The purpose of the study is to develop new biguanides antihyperglycemic drugs and interpret their possible structure-activity relationship(SAR). By studying the structural characteristics of various substituents on N1 of biguanides, we designed and synthesized five new biguanides compounds under high temperature. We investigated the effects of the synthesized compounds on the blood glucose of type II diabetes rats. Our major results are as follows:1. Preparation and identification of the new biguanides Equimolar mixtures of amino acid ester hydrochloride and dicyandiamide at fusion temperatures were reacted in a suitable time respectively. The products were rinsed with aether and decolored with Activated Charcoal. The final products were obtained by recrystallization in methanol. The final products with purity of above 98% were determined using HPLC, and the chemical structures of these compounds were identified using C13 and H spectrum of NMR.2. The effects of synthesized new biguanides on the blood glucose of...