Effect of a novel succinamic acid derivative as potential anti-diabetic agent in experimental diabetic rats

4-((benzyloxy) amino)-2-hydroxy-4-oxobutanoic acid which is a succinamic acid derivative has been synthesized in 3 step reaction with malic acid. Its structure confirmation was done by various techniques like 1H NMR, 13C NMR, & HRMS and is recently proposed as an insulinotropic agent for the treatment of non-insulin dependent diabetes mellitus. In the present study, the effect of 4-((benzyloxy) amino)-2-hydroxy-4-oxobutanoic acid on plasma glucose, serum insulin, serum lipid profile and lipid peroxidation in streptozotocin–nicotinamide induced type 2 diabetic model was investigated.  4-((benzyloxy) amino)-2-hydroxy-4-oxobutanoic acid was administered orally (20 mg/kg b.w.) to streptozotocin + nicotinamide (STZ + NAD) induced diabetic rats for 28 days. A significant increase in fasting blood glucose levels, HbA1c levels, Serum lipid profile (TG & TC) and in  the levels of Malonaldialdehyde (MDA, end product of lipid peroxidation) was observed in STZ +NAD diabetic rats whereas the levels of high density lipoprotein-cholesterol (HDL-C) and serum insulin levels were significantly decreased  in STZ + NAD induced diabetic rats The effect of 4-((benzyloxy)amino)-2-hydroxy-4-oxobutanoic acid was compared with glibenclamide, a reference drug. Treatment with 4-((benzyloxy) amino)-2-hydroxy-4-oxobutanoic acid and glibenclamide resulted in a significant reduction of fasting blood glucose levels with increase in plasma insulin levels in diabetic treated rats. 4-((benzyloxy) amino)-2-hydroxy-4-oxobutanoic acid also resulted in a significant improvement in serum lipids and lipid peroxidation products. Our results suggest the potential role of 4-((benzyloxy) amino)-2-hydroxy-4-oxobutanoic acid in the management of type-2 diabetes mellitus experimental rats. Keywords: 4-((benzyloxy) amino)-2-hydroxy-4-oxobutanoic acid, dyslipidemia, streptozotocin induced diabetes, lipid peroxidatio

Eco-friendly reactions in PEG-400: a highly efficient and green approach for stereoselective access to multisubstituted 3,4-dihydro-2(1<i>H</i>)-quinazolines using 2-aminobenzylamines

An efficient, green and stereoselective synthesis of multisubstituted 3,4-dihydro-2(1H)-quinazolines using PEG-400 as an inexpensive and non-toxic reaction medium is reported.</p

Extraction and analysis of nicotine (3-(1-methyl-2-pyrrolidinyl)pyridine) from cigarettes using small volume liquid extraction and ultrasonic bath system technique

The tobacco (Nicotiana tabacum) plant belongs to solanaceae family. It is an annual herbaceous plant. Over 0.45 million hectares of land are used for growing tobacco commercially, with a total production of over 750 million kg of tobacco. According to the Global adult tobacco survey held in the year 2016-2017, there are nearly 267 million adults (above 15 years of age) in India abusing tobacco. Nicotine can be extracted from biological samples by liquid-liquid extraction, small volume liquid extraction, etc. Thin-layer chromatography is a very effective technique as it can be employed for many samples simultaneously, which is cost-effective and easy to perform without any errors. A new technique, the Ultrasonic bath technique (Sonication technique) is used for the same. Four different types of solvents were used for extraction purposes out of which two gave favorable results. This methodology is proven to be cost-effective, consumes fewer chemicals, less manpower, and is effective.<jats:p /

Recent Advances in Development of GPR40 Modulators (FFA1/FFAR1): An Emerging Target for Type 2 Diabetes

Background: GPR40, an orphan G-protein coupled receptor that is activated by medium and long-chain fatty acids and is highly expressed in pancreatic islets, adipose depots and the gastrointestinal tract are involved in energy source recognition, absorption, storage and/or metabolism. Since its deorphanization in 2003, G-protein-coupled receptor GPR40 has emerged as a potential target for type II diabetes because it has been hypothesized to participate in the adverse effects of chronic fatty acid exposure on function of β-cell. &lt;/p&gt; &lt;p&gt; Results: This signifies that G-protein-coupled receptors have recently emerged as novel therapeutic targets in metabolic diseases, such as diabetes, obesity and the metabolic syndrome. Therefore it seems natural that GPR40 represents a potentially attractive target to best meet the need for novel treatments for Type II diabetes. &lt;/p&gt; &lt;p&gt; Conclusion: This review describes recent advances and novel drug discovery approaches in the antidiabetic area, focusing on GPR40 modulators which have been synthesized till date and their Structure-Activity Relationship (SAR). </jats:sec