[reaction: see text] Catalyst-free conjugate addition of thiols to alpha,beta-unsaturated carbonyl compounds in water is reported. beta-Sulfido carbonyl compounds were formed at room temperature, in short times and with excellent chemoselectivity. Competitive dithiane/dithiolane formation, transesterification, and ester cleavage were not observed. Water played a dual role in simultaneously activating the alpha,beta-unsaturated carbonyl compound and the thiol. This new methodology constitutes an easy, highly efficient, and green synthesis of beta-sulfido carbonyl compounds.
Background:
Among the millions of people around the world, the most prevalent metabolic
disorder is diabetes mellitus. Due to the drawbacks which are associated with commercially available
antidiabetic agents, new therapeutic approaches are needed to be considered. Alpha-amylase is a membrane-
bound enzyme which is responsible for the breakdown of polysaccharides such as starch to
monosaccharides which can be absorbed.
Methods:
We searched the scientific database using alpha-amylase, diabetes, antidiabetic agents as the
keywords. Here in, only peer-reviewed research articles were collected which were useful to our current
work.
Results:
To overcome the research gap, the alpha-amylase enzyme is regarded as a good target for antidiabetic
agents to design the drug and provide an alternate approach for the treatment of type 2 diabetes
mellitus. Basically, alpha-amylase inhibitors are classified into two groups: proteinaceous inhibitors,
and non-proteinaceous inhibitors. Recently, non-proteinaceous inhibitors are being explored
which includes chalcones, flavones, benzothiazoles, etc. as the potential antidiabetic agents.
Conclusion:
Herein, we discuss various potential antidiabetic agents which are strategically targeted
alpha-amylase enzyme. These are having lesser side effects as compared to other antidiabetic agents,
and are proposed to prevent the digestion and absorption of glucose leading to a decrease in the blood
glucose level.
The incidence of diabetes has increased globally in recent years and figures of diabetic patients were estimated to rise up to 642 million by 2040. The disorder is accompanied with various complications if not managed at the early stages, and interlinked high mortality rate and morbidity with time. Different classes of drugs are available for the management of type 2 diabetes but were having certain limitations of their safety. Alphaglucosidase is a family of enzyme originated from the pancreas which plays a role in the anabolism of 80-90% of carbohydrate consumed into glucose. This glucose is absorbed into the blood and results in frank postprandial hyperglycemia and worsens the conditions of diabetic patients which precipitate complications. Inhibition of these enzymes helps to prevent postprandial hyperglycemia and the formation of glycated end products. Alphaglucosidase inhibitors are reported to be more important in adequate control of type 2, but marketed drugs have various side effects, such as poor patient compliance and also expensive. This proves the needs for other class of drugs with better efficacy, safety, patient compliance and economic. In this review, we have emphasized the recent advances in the field of new alpha-glucosidase inhibitors with improved safety and pharmacological profile.
Synergistic effects of the exo- and endocyclic chiral centers of an imidazolidinone-based auxiliary were investigated in the perspective of acetate aldol reactions. The reversal in diastereoselectivity was accomplished by lithium and titanium enolate reactions, which proceed through proposed open and closed transitions states, respectively. The aldol adducts were used in the stereoselective synthesis of fluoxetine.
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