Structural Basis for the Structure-Activity Relationships of Peroxisome Proliferator-Activated Receptor Agonists

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• 作者：Neeraj Mahindroo ; Yi-Hui Peng ; Chia-Hui Lin ; Uan-Kang Tan ; Ekambaranellore Prakash ; Tzu-Wen Lien ; I-Lin Lu ; Hong-Jen Lee ; John Tsu-An Hsu ; Xin Chen ; Chun-Chen Liao ; Ping-Chiang Lyu ; Yu-Sheng Chao ; Su-
• 刊名：Journal of Medicinal Chemistry
• 出版年：2006
• 出版时间：October 19, 2006
• 年：2006
• 卷：49
• 期：21
• 页码：6421 - 6424
• 全文大小：152K
• 年卷期：v.49,no.21(October 19, 2006)
• ISSN：1520-4804

文摘

Type 2 diabetes has rapidly reached an epidemic proportion becoming a major threat to global public health.PPAR agonists have emerged as a leading class of oral antidiabetic drugs. We report a structure biologyanalysis of novel indole-based PPAR agonists to explain the structure-activity relationships and present acritical analysis of reasons for change in selectivity with change in the orientation of the same scaffolds.The results would be helpful in designing novel PPAR agonists.