Design, synthesis, and biological evaluation of novel thiazolidinediones as PPARγ/FFAR1 dual agonists
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- 作者：Khaled M. Darwish ; Ismail Salama ; Samia Mostafa ; Mohamed S. Gomaa ; Mohamed A. Helal ; mohamed_hilal@pharm.suez.edu.eg" class="auth_mail" title="E-mail the corresponding author
- 关键词：Diabetes ; PPARγ ; FFAR1 ; Thiazolidinedione ; Docking
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：15 February 2016
- 年：2016
- 卷：109
- 期：Complete
- 页码：157-172
- 全文大小：2087 K
文摘
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PPARγ and FFAR1 are valid targets for the management of type 2 diabetes.
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Some thiazolidinediones (PPAR ligands) could activate FFAR1 with micromolar potency.
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In this study, nineteen dual PPARγ/FFAR1 agonists were designed.
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The design depends on using TZD head with diverse privileged structures.
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Nine compounds showed promising dual activity.