Synthesis and antidiabetic evaluation of some novel compounds

Aryloxypropanolmines have been reported to have beta(3)-agonist activity. Agonists of beta(3)-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 targe...

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Published inIndian journal of chemistry. Sect. B. Organic chemistry, including medicinal chemistry Vol. 58; no. 7; pp. 849 - 854
Main Authors Avalakki, Anagha S., Jadhav, Shailaja B., Bandawane, Deepti D., Bhalekar, Pournima A.
Format Journal Article
LanguageEnglish
Published NEW DELHI Natl Inst Science Communication & Information Resources-Niscair 01.07.2019
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
streptozotocin
Aryloxypropanolamines
lipolysis
BETA-ADRENERGIC RECEPTORS
glibenclamide
antidiabetic activity
ADIPOSE-TISSUE
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Summary:Aryloxypropanolmines have been reported to have beta(3)-agonist activity. Agonists of beta(3)-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.
ISSN:0376-4699
0019-5103