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Volumn 21, Issue 8, 2011, Pages 2345-2350

Phenoxyacetic acids as PPARδ partial agonists: Synthesis, optimization, and in vivo efficacy

Author keywords

Partial agonist; PPARd

Indexed keywords

PARTIAL AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA AGONIST; PHENOXYACETIC ACID DERIVATIVE;

EID: 79953278556     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.02.077     Document Type: Article
Times cited : (8)

References (23)
  • 13
    • 79953282674 scopus 로고    scopus 로고
    • 3 buffer 0.5/99.5 pH 10
    • 3 buffer 0.5/99.5 pH 10.
  • 18
    • 79953267496 scopus 로고    scopus 로고
    • 2, 140 bar, 40 °C, 2 mL/min on an AS column monitored at 215 nm. (S)-3a, 95% ee, 87% pure and (R)-3b, 98% ee, 93% pure
    • 2, 140 bar, 40 °C, 2 mL/min on an AS column monitored at 215 nm. (S)-3a, 95% ee, 87% pure and (R)-3b, 98% ee, 93% pure.
  • 19
    • 79953268853 scopus 로고    scopus 로고
    • free = 23.6%, PDB code 3PEQ
    • free = 23.6%, PDB code 3PEQ.
  • 20
    • 79953274186 scopus 로고    scopus 로고
    • note
    • Distances reported are the average distances from the residues in the crystal structure of 48 bound to PPARd which has two subunits. Compounds 3a and 3b were overlaid into both subunits, with the (S)-methyl of 3a lying 2.01 and 2.26 from Thr289 in the two subunits, and with the (R)-methyl of 3b lying 2.78 and 2.93 from Leu469 in the two subunits.
  • 22
    • 79953275636 scopus 로고    scopus 로고
    • All animal studies were conducted after review by the GSK Institutional Animal Care and Use Committee and in accordance with the GSK Policy on the Care, Welfare and Treatment of Laboratory Animals
    • All animal studies were conducted after review by the GSK Institutional Animal Care and Use Committee and in accordance with the GSK Policy on the Care, Welfare and Treatment of Laboratory Animals.
  • 23
    • 79953291941 scopus 로고    scopus 로고
    • ob/ob mice, 6 weeks of age. Positive control: GW610742X (30 mg/kg). Vehicle: HPMC/Tween. Compound dosed orally (10, 30, 100 mg/kg) once daily for 15 days. OGTT performed on fasted animals at day 12 of dosing
    • ob/ob mice, 6 weeks of age. Positive control: GW610742X (30 mg/kg). Vehicle: HPMC/Tween. Compound dosed orally (10, 30, 100 mg/kg) once daily for 15 days. OGTT performed on fasted animals at day 12 of dosing.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.