Linked Life Data

21720040

Source:http://linkedlifedata.com/resource/pubmed/id/21720040

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
7
pubmed:dateCreated
2011-7-1
pubmed:abstractText
2-Acyl-tetrahydroisoquinoline-3-carboxylic acid derivatives were synthesized and biologically evaluated. (S)-2-(2,4-Hexadienoyl)-7-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (14) showed peroxisome proliferator-activated receptor ? (PPAR?) and PPAR? agonist activities and protein-tyrosine phosphatase 1B (PTP-1B) inhibitory activities. PPAR? agonist activity of 14 was comparable to that of rosiglitazone, and PTP-1B inhibitory activity was about 10-fold weaker than that of ertiprotafib, a PTP-1B inhibitor. Compound 14 showed high oral absorption in rats and potent hypoglycemic effects in KK-A(y) mice. In conclusion, 14 would be an excellent lead compound for a new type of anti-diabetic drug with triple actions.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1347-5223
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
59
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
876-9
pubmed:meshHeading
pubmed:year
2011
pubmed:articleTitle
2-Acyl-tetrahydroisoquinoline-3-carboxylic acids: lead compounds with triple actions, peroxisome proliferator-activated receptor ?/? agonist and protein-tyrosine phosphatase 1B inhibitory activities.
pubmed:affiliation
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd., Nakagyo-ku, Kyoto, Japan.
pubmed:publicationType
Journal Article