Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 3, Pages 1348-1351Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.12.066
Keywords
(-)-Cercosporamide; Diabetes; PPAR gamma modulator; SPPARM; SPPAR gamma M
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Peroxisome proliferator-activated receptor gamma (PPAR gamma) is a potential drug target for treating type 2 diabetes. The selective PPAR gamma modulators (SPPARMs), which partially activate the PPAR gamma transcriptional activity, are considered to improve the plasma glucose level with attenuated PPAR gamma related adverse effects. However, the relationships between desired pharmacological profiles and ligand specific PPAR gamma transcriptional profiles have been unclear. And there is also little knowledge of how to control ligand specific PPAR gamma transcriptional profiles. Herein, we present synthesis of novel derivatives containing substituent at naphthalene C3 position of compound 1. The novel derivatives showed various maximal efficacies as PPAR gamma partial agonist. (C) 2011 Elsevier Ltd. All rights reserved.
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