Bioorganic & Medicinal Chemistry Letters 2001-11-19

Identification of a series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis.

K G Liu, M H Lambert, L M Leesnitzer, W Oliver, R J Ott, K D Plunket, L W Stuart, P J Brown, T M Willson, D D Sternbach

Index: Bioorg. Med. Chem. Lett. 11(22) , 2959-62, (2001)

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Abstract

We have developed a general solid-phase synthesis for identification of PPAR ligands. Synthesis of a 480-member library led to the identification of a potent PPAR gamma/delta dual agonist 23. Compound 23 showed good plasma exposure in rats and demonstrated antihyperglycemic and antihyperlipidemic efficacy in diabetic fatty Zucker rats.