Design, synthesis, and evaluation of tetrahydroquinoline-linked thiazolidinedione derivatives as ppar gamma selective activators

초록

A series of tetrahydroquinoline-linked thiazolidinediones was designed and synthesized and their peroxisome proliferator activated receptor-gamma (PPAR gamma) agonistic activities were evaluated. A number of analogs were revealed to have significant PPAR gamma agonistic activity. Among these compounds, compound 1h possessing N-heptyl moiety was found to be the most active in PPAR gamma transactivation assay. Molecular modeling suggested that the heptyl group of 1h appropriately interacts with hydrophobic amino acid residues in the active site of PPAR gamma.

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