Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2 |
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Authors: | Usui Shinya Suzuki Takayoshi Hattori Yoshifumi Etoh Kazuma Fujieda Hiroki Nishizuka Makoto Imagawa Masayoshi Nakagawa Hidehiko Kohda Kohfuku Miyata Naoki |
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Institution: | Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan. |
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Abstract: | To develop novel PPARgamma ligands, we synthesized thirteen 3-{4-(2-aminoethoxy)phenyl}propanoic acid derivatives, which are designed based on the structures of rosiglitazone and 15d-PGJ2. Among these compounds, compound 9 was found to be as potent as rosiglitazone in a binding assay and a preadipocyte differentiation test. Molecular modeling suggested that the nonyl group of 9 interacted with hydrophobic amino acid residues constructing the hydrophobic region of PPARgamma protein where the alkyl chain of 15d-PGJ2 is expected to be located. |
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