Flavone-Based Novel Antidiabetic and Antidyslipidemic Agents
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- 作者：Alok K. Verma ; Himanshu Singh ; Mavurapu Satyanarayana ; Swayam P. Srivastava ; Priti Tiwari ; Amar B. Singh ; Anil K. Dwivedi ; Shio K. Singh ; Mukesh Srivastava ; Chandishwar Nath ; Ram Raghubir ; Arvind K. Srivastava ; Ram Pratap
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：May 24, 2012
- 年：2012
- 卷：55
- 期：10
- 页码：4551-4567
- 全文大小：657K
- 年卷期：v.55,no.10(May 24, 2012)
- ISSN：1520-4804
文摘
The hybrid congeners 62鈥?b>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.