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Synthesis and antidiabetic evaluation of some novel compounds

By: Avalakki, Anagha S.
Contributor(s): Jadhav, Shailaja B.
Publisher: New Delhi CSIR 2019Edition: Vol.58(B), July.Description: 849-854p.Subject(s): GENERAL CHEMISTRYOnline resources: Click here In: Indian journal of chemistry (Section B)Summary: Aryloxypropanolmines have been reported to have β3-agonist activity. Agonists of β3-adrenergic receptors have been observed to simultaneously increase lipolysis, fat oxidation, energy expenditure and insulin action leading to the belief that this receptor might serve as an attractive target for the treatment of diabetes and obesity. Various aryloxypropanolamine derivatives have been synthesized starting with the substituted imines derived from 4-hydroxy benzaldehyde and substituted anilines. These imines have been converted to benzamide intermediates. The benzamide epoxide intermediates have been synthesized using epichlorhydrin. The title compounds 6a-j have been synthesized via ring opening of the epoxides. The synthesized compounds have been characterized using infrared (IR), nuclear magnetic resonance (NMR) and mass spectrometry. The synthesized compounds have been evaluated for antidiabetic activity on streptozotocin induced diabetic male Wistar rats. The synthesized aryloxypropanolamine derivative consisting of –OCH3 and t-butyl amine substituents show good activity as compared to the other synthesized compounds in the series. Glibenclamide has been taken as standard for measuring the antidiabetic activity.
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Aryloxypropanolmines have been reported to have β3-agonist activity. Agonists of β3-adrenergic receptors have been observed to simultaneously increase lipolysis, fat oxidation, energy expenditure and insulin action leading to the belief that this receptor might serve as an attractive target for the treatment of diabetes and obesity. Various aryloxypropanolamine derivatives have been synthesized starting with the substituted imines derived from 4-hydroxy benzaldehyde and substituted anilines. These imines have been converted to benzamide intermediates. The benzamide epoxide intermediates have been synthesized using epichlorhydrin. The title compounds 6a-j have been synthesized via ring opening of the epoxides. The synthesized compounds have been characterized using infrared (IR), nuclear magnetic resonance (NMR) and mass spectrometry. The synthesized compounds have been evaluated for antidiabetic activity on streptozotocin induced diabetic male Wistar rats. The synthesized aryloxypropanolamine derivative consisting of –OCH3 and t-butyl amine substituents show good activity as compared to the other synthesized compounds in the series. Glibenclamide has been taken as standard for measuring the antidiabetic activity.

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