- Synthesis and evaluation of a series of benzopyran derivatives as PPAR α/γ agonists
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A series of benzopyran derivatives were synthesized and evaluated for PPAR α/γ agonist activities. Most of the compounds exhibit reasonable PPAR α and PPAR γ agonist activities. In particular, compounds 7b, 8b, 8e and 8h with remarkable PPARg EC50 values of 0.001 μM are excellent full PPAR γ agonists with the functional potency about 130, 20 times stronger than that of leading compound 5 and rosiglitazone, respectively. Compounds 7a, 7c, 7d and 8a are dual PPAR α/γ agonists, and all of them gave comparable or stronger PPAR α/γ agonist efficacy than that of the corresponding positive control.
- Yu, Juanhong,Tang, Lei,Yang, Yushe,Ji, Ruyun
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p. 2428 - 2435
(2008/12/23)
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- Azole phenoxy hydroxyureas as selective and orally active inhibitors of 5- lipoxygenase
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Azole phenoxy hydroxyureas are a new class of 5-lipoxygenase (5-LO) inhibitors. Structure-activity relationship studies have demonstrated that electronegative substituents on the 2-phenyl portion of the oxazole tail increased the ex vivo potency of these
- Malamas,Carlson,Grimes,Howell,Glaser,Gunawan,Nelson,Kanzelberger,Shah,Hartman
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p. 237 - 245
(2007/10/03)
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