Structural Basis for the Structure−Activity Relationships of Peroxisome Proliferator-Activated Receptor Agonists
Journal of Medicinal Chemistry2006Vol. 49(21), pp. 6421–6424
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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‐Ying Wu, Hsing‐Pang Hsieh
Abstract
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 biology analysis of novel indole-based PPAR agonists to explain the structure-activity relationships and present a critical 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.
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