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Synthesis and Biological Evaluation of Some Novel Keto-Sulfones Derivatives as Antidiabetic Agents.
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| Author:
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UPLOADED BY-ADMIN, SHASHANK TRIVEDI, PRAKASH PATIDAR, R.S. PAWAR, P.K. SINGOUR, U.K. PATIL
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| Abstract:
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Peroxisome proliferators-activated receptor-? (PPAR?) and 11?-hydroxysteroid dehydroge- nase type 1(11?-
HSD1) are two novel molecular therapeutic targets for type 2 diabetes by increasing insulin sensitivity and improving glycemic
control. The ?- keto sulfones derivatives were discovered as potent and selective 11 ?-HSD1 inhibitors. A detailed
enzymatic study revealed that ?-keto sulfones are the substrate of 11?-HSD1 enzyme. They inhibit by competing with substrate
for the active site, they are then turned over by the enzyme to products which are not inhibitors. Therefore, here we
had tried to synthesize some of the novel keto-sulfones derivatives and tested them for their antidiabetic activity. The structures
of the compound have been confirmed by spectral analysis. Newly synthesized compounds were tested for antihyperglycemic
activity using Alloxan induced diabetic model. Among the synthesized compounds 1-(3,4-dimethoxyphenyl)-2-
(thiophen-2-ylsulfonyl) ethanone (5e) were found to be most active with the percent change in plasma glucose level of
16.70 after 24 hours.
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| Keyword:
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Keto-sulfones, type 2 diabetes, 11?-HSD1 Inhibitors
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| EOI:
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| DOI:
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