rdf:type |
|
lifeskim:mentions |
umls-concept:C0023688,
umls-concept:C0166418,
umls-concept:C0221874,
umls-concept:C0337112,
umls-concept:C0449560,
umls-concept:C0597357,
umls-concept:C0599740,
umls-concept:C0772162,
umls-concept:C0991876,
umls-concept:C1260969,
umls-concept:C1524075,
umls-concept:C1704737,
umls-concept:C1709059
|
pubmed:issue |
24
|
pubmed:dateCreated |
2008-11-25
|
pubmed:abstractText |
Oxazole containing glycine and oximinobutyric acid derivatives were synthesized as PPARalpha agonists by incorporating polymethylene spacer as a replacement of commonly used phenylene group that connects the acidic head with lipophilic tail. Compound 13a was found to be a selective and potent PPARalpha agonist. Further 1,3-dioxane-2-carboxylic acid derivative 20 was synthesized by replacing the tetramethylene spacer of NS-220, a selective PPARalpha agonist with phenylene group and found to exhibit PPARalpha/gamma dual agonism. These results suggest that compounds possessing polymethylene spacer between pharmacophore and lipophilic tail exhibit predominantly PPARalpha agonism whereas those with an aromatic phenylene spacer shows PPARalpha/gamma dual agonism.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
1464-3405
|
pubmed:author |
pubmed-author:GoelAshishA,
pubmed-author:JainMukulM,
pubmed-author:JamiliJeevankumarJ,
pubmed-author:MakadiaPankajP,
pubmed-author:PatelMeghaM,
pubmed-author:PatelPankajP,
pubmed-author:PatilPravinP,
pubmed-author:PingaliHarikishoreH,
pubmed-author:SairamKalapatapu V V MKV,
pubmed-author:ShahShaileshS,
pubmed-author:ZawarePandurangP
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
18
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
6471-5
|
pubmed:meshHeading |
pubmed-meshheading:18976908-Butyric Acids,
pubmed-meshheading:18976908-Chemistry, Pharmaceutical,
pubmed-meshheading:18976908-Dioxanes,
pubmed-meshheading:18976908-Drug Design,
pubmed-meshheading:18976908-Glycine,
pubmed-meshheading:18976908-Humans,
pubmed-meshheading:18976908-Hydrogen,
pubmed-meshheading:18976908-Hydrogen Bonding,
pubmed-meshheading:18976908-Ligands,
pubmed-meshheading:18976908-Models, Chemical,
pubmed-meshheading:18976908-Oxazoles,
pubmed-meshheading:18976908-PPAR alpha,
pubmed-meshheading:18976908-Peroxisome Proliferator-Activated Receptors,
pubmed-meshheading:18976908-Transcriptional Activation
|
pubmed:year |
2008
|
pubmed:articleTitle |
Modulation of PPAR receptor subtype selectivity of the ligands: aliphatic chain vs aromatic ring as a spacer between pharmacophore and the lipophilic moiety.
|
pubmed:affiliation |
Zydus Research Centre, Sarkhej-Bavla N.H. No. 8A, Moraiya, Ahmedabad, Gujarat 382210, India. pingalihk@rediffmail.com
|
pubmed:publicationType |
Journal Article
|