Flavone-Based Novel Antidiabetic and Antidyslipidemic Agents

The hybrid congeners 62–90 of 6- and 7-hydroxyflavones with aminopropanol have been synthesized and evaluated for their antidiabetic activity in sucrose-challenged low-dosed streptozotocin (STZ)-induced diabetic rats and db/db mice. The optical enantiomers 70a, 70b, 90a, and 90b of two congeners 70...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2012-05, Vol.55 (10), p.4551-4567
Main Authors: Verma, Alok K, Singh, Himanshu, Satyanarayana, Mavurapu, Srivastava, Swayam P, Tiwari, Priti, Singh, Amar B, Dwivedi, Anil K, Singh, Shio K, Srivastava, Mukesh, Nath, Chandishwar, Raghubir, Ram, Srivastava, Arvind K, Pratap, Ram
Format: Article
Language:English
Subjects:
Animals
Biological Availability
Cholesterol - blood
Cricetinae
Diabetes Mellitus, Experimental - drug therapy
Dose-Response Relationship, Drug
Flavones - chemical synthesis
Flavones - chemistry
Flavones - pharmacology
Hypoglycemic Agents - chemical synthesis
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacology
Hypolipidemic Agents - chemical synthesis
Hypolipidemic Agents - chemistry
Hypolipidemic Agents - pharmacology
Insulin - blood
Male
Mesocricetus
Mice
Mice, Inbred C57BL
Rats
Rats, Sprague-Dawley
Rats, Wistar
Stereoisomerism
Streptozocin
Structure-Activity Relationship
Triglycerides - blood
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Summary:The hybrid congeners 62–90 of 6- and 7-hydroxyflavones with aminopropanol have been synthesized and evaluated for their antidiabetic activity in sucrose-challenged low-dosed streptozotocin (STZ)-induced diabetic rats and db/db mice. The optical enantiomers 70a, 70b, 90a, and 90b of two congeners 70 and 90 exhibiting consistent antidiabetic and antidyslipidemic activities were also prepared, and their antidiabetic activity results indicate its association mainly with S isomers. These compounds also lower cholesterol and TG profiles while improving high-density lipoprotein cholesterol to CHOL ratio in db/db mice. The bioavailability of compound 70 and its isomer varies between 27 and 29% whereas that of the more polar compound 90a is poor as determined in rat by oral and intraperitoneal administrations.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm201107g