Synthesis of propiophenone derivatives as new class of antidiabetic agents reducing body weight in db/db mice

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• 作者：Atul Kumar^a ; ^{dratulsax@gmail.com} ; Siddharth Sharma^a ; Lalit Prakash Gupta^a ; Pervez Ahmad^a ; Swayam Prakash Srivastava^b ; Neha Rahuja^b ; A.K. Tamrakar^b ; Arvind K. Srivastava^b
• 关键词：Propiophenone ; Antidiabetic ; PTP-1B ; db/db Mice ; Body weight
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 March, 2012
• 卷：20
• 期：6
• 页码：2172-2179
• 文件大小：766 K

摘要

A series of propiophenone derivatives (6-23) have been synthesized and evaluated for their in vivo antihyperglycemic activities in sucrose loaded model (SLM), sucrose challenged streptozotocin (STZ-S) induced diabetic rat model and C57BL/KsJ db/db diabetic mice model. Compound 15 and 16 were emerged as potent antihyperglycemics and lipid lowering agents. These compounds (15, 16) further validate the potency by reducing body weight and food intake in db/db mice model. Possible mechanism of action for the propiophenone derivatives was established by the evaluation in various in vitro models. Interestingly some of the compounds were efficiently inhibiting PTP-1B.