Abstract
Three of imide intermediate products were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c) respectively in dry toluene with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the resulted products consider as the end products (5a-j) while the compounds (5k-o) required further reaction to deprotect aliphatic amine this achieved by treating the compounds with TFA to remove tert-Butoxycarbonyl group (6a-e).
 The alpha glucosidase inhibitory activity of some synthesized compounds (5a, 5f, 6a) were tested by using -glucosidase from Saccharomyces cerevisiae, p-nitrophenol glucopyranoside (pNPG) used as substrate and acarbose used as standard.
 All these test compounds shows excellent inhibitory activity according to IC50 values which is ranging from (4.61-7.32).
Highlights
IntroductionInsulin is a peptide hormone produced by beta cells of the pancreas [2].It hastwo essential functions: [1] insulin stimulates glucoseuptake and lipid synthesis; [2] insulin inhibits the breakdown of lipids, proteins and glycogen, and inhibits the glucose biosynthesis pathway (gluconeogenesis) [4,5,6]
Diabetes mellitus (DM) is a chronic metabolic disorder with heterogeneous etiologies )genetic and environmental factors(, it is characterized by disturbance in the metabolisms of carbohydrate, fat and protein resulting from defects in insulin secretion, insulin action or both[1,2,3]
In type-2 diabetes, the body does not produce enough insulin for proper functioning orthe cells do not react to insulin [8].As type 2 diabetes is a progressivedisease, intensification of therapy is normally required over time, traditional treatmentalgorithms oftenfail to address the progressive nature of the disease.current therapeutic agents may be associated with wide range of various effects: increased risk of hypoglycemia, weight gain, and gastrointestinal intolerance, which representbarriers to maximum glycemic control[9,10,11]
Summary
Insulin is a peptide hormone produced by beta cells of the pancreas [2].It hastwo essential functions: [1] insulin stimulates glucoseuptake and lipid synthesis; [2] insulin inhibits the breakdown of lipids, proteins and glycogen, and inhibits the glucose biosynthesis pathway (gluconeogenesis) [4,5,6]. In type-2 diabetes, the body does not produce enough insulin for proper functioning orthe cells do not react to insulin (insulin resistance) [8].As type 2 diabetes is a progressivedisease, intensification of therapy is normally required over time, traditional treatmentalgorithms oftenfail to address the progressive nature of the disease.current therapeutic agents may be associated with wide range of various effects: increased risk of hypoglycemia (sulphonylureas and insulin), weight gain (sulphonylureas, thiazolidinediones and insulin), and gastrointestinal intolerance (metformin), which representbarriers to maximum glycemic control[9,10,11].
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Schedule a callMore From: Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512)
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