CITRACONIC ACID ISONICOTINOYLHYDRAZIDE ELICITING HYPOGLYCAEMIC ACTIVITY Russian patent published in 2002 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to the class of dicarboxylic acid hydrazides, namely to a novel biologically active citraconic acid isonicotinoylhydrazide of the formula: . Compound is synthesized by interaction of isonicotinic acid with citraconic anhydride. Compound is a white crystalline substance, soluble in water, ethanol, dimethylformamide (DMFA) with value T_m = 103-104 C ((d)). Compound shows hypoglycaemic activity decreasing blood sugar level in healthy rats after intraperitoneal administration in the dose 50 mg/kg by 34.6 ± 2.4% in 3 h and by 29.9 ± 6.9% in 5 h; after peroral administration in rats with alloxan diabetes mellitus model the compound decreases blood glucose level by 41.3 ± 3.0% in 3 h and by 37.7 ± 3.2% in 5 h. Value LD₅₀ at an intraperitoneal administration in white mice is equal 410 (350-470) mg/kg. EFFECT: new compound indicated above, valuable antidiabetic properties. 1 tbl