rdf:type |
|
lifeskim:mentions |
umls-concept:C0023688,
umls-concept:C0166417,
umls-concept:C0205314,
umls-concept:C0205460,
umls-concept:C0220781,
umls-concept:C0289313,
umls-concept:C0441655,
umls-concept:C0679622,
umls-concept:C1312096,
umls-concept:C1527178,
umls-concept:C1705938,
umls-concept:C1707689,
umls-concept:C1883254
|
pubmed:issue |
6
|
pubmed:dateCreated |
2005-3-4
|
pubmed:abstractText |
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.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
0960-894X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
15
|
pubmed:volume |
15
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1547-51
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:15745794-Adipocytes,
pubmed-meshheading:15745794-Animals,
pubmed-meshheading:15745794-Cells, Cultured,
pubmed-meshheading:15745794-Drug Design,
pubmed-meshheading:15745794-Ligands,
pubmed-meshheading:15745794-Models, Molecular,
pubmed-meshheading:15745794-Molecular Structure,
pubmed-meshheading:15745794-PPAR gamma,
pubmed-meshheading:15745794-Prostaglandin D2,
pubmed-meshheading:15745794-Protein Binding,
pubmed-meshheading:15745794-Rats,
pubmed-meshheading:15745794-Thiazolidinediones
|
pubmed:year |
2005
|
pubmed:articleTitle |
Design, synthesis, and biological activity of novel PPARgamma ligands based on rosiglitazone and 15d-PGJ2.
|
pubmed:affiliation |
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|