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Volumn 17, Issue 15, 2007, Pages 4144-4149

Novel selective PPARδ agonists: Optimization of activity by modification of alkynylallylic moiety

Author keywords

Hydroalumination; Nuclear receptor; Peroxisome proliferator activated receptor ; PPAR agonists; Substituted allyl alcohols

Indexed keywords

PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA;

EID: 34447122589     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.05.051     Document Type: Article
Times cited : (12)

References (28)
  • 3
    • 85119818273 scopus 로고    scopus 로고
    • A unified nomenclature system for the nuclear receptor superfamily. Cell 1999, 97, 161.
  • 16
    • 34447120352 scopus 로고    scopus 로고
    • note
    • 2 (30 mg, 0.042 mmol) were added; the reaction mixture was degassed again and then stirred under inert atmosphere at 65 °C. The reaction was monitored by TLC....
  • 19
    • 34447136315 scopus 로고    scopus 로고
    • note
    • 3P in cyclohexane (0.15 M, 0.40 mL, 0.060 mmol) were added. The reaction mixture was stirred at 50 °C for 90 min, cooled down, and 10% aqueous solution of potassium fluoride was added. The mixture was stirred for 10 min, filtered through a pad of silica gel and the silica gel was washed with ethyl acetate (50 mL). The filtrate was washed with brine (3 × 15 mL), 10% aqueous solution of potassium fluoride (2 × 10 mL), water (2 × 10 mL), and brine (3 × 15 mL). The organic solution was dried with sodium sulfate, concentrated and purified by flash column chromatography (silica gel, hexanes/ethyl acetate 10:1). The crude product was triturated with hexanes/ethyl acetate mixture (15:1, 16 mL) yielding methyl (Z)-[2-methyl-4-[3-[4-(5-methylthiophen-2-yl)phenyl]-5-phenylpent-2- en-4-ynyloxy]phenoxy] acetate (14n) as a yellowish amorphous mass in 47% yield.
  • 25
    • 34447123402 scopus 로고    scopus 로고
    • PPAR in-vitro transactivation assay was performed as described in Ref. 11.
  • 26
    • 34447123401 scopus 로고    scopus 로고
    • note
    • 27,28 6f was built in Maestro version 7.5, a formal charge of -1 was assigned, and the molecule was minimized with the OPLS_2005 force field. 6f was docked with Glide version 4.0 using the SP mode and the van der Waals radii of the ligand atoms were scaled by 0.8.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.