Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.

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Mogensen JP, Jeppesen L, Bury PS, Pettersson I, Fleckner J, Nehlin J, Frederiksen KS, Albrektsen T, Din N, Mortensen SB, Svensson LA, Wassermann K, Wulff EM, Ynddal L, Sauerberg P

Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.

Bioorg Med Chem Lett. 2003 Jan 20;13(2):257-60.

PubMed ID
12482434 [ View in PubMed
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Abstract

Using a known dual PPARalpha/gamma activator (5) as a structural template, SAR evaluations led to the identification of triple PPARalpha/gamma/delta activators (18-20) with equal potency and efficacy on all three receptors. These compounds could become useful tools for studying the combined biological effects of PPARalpha/gamma/delta activation.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
(2S)-2-ETHOXY-3-{4-[2-(10H-PHENOXAZIN-10-YL)ETHOXY]PHENYL}PROPANOIC ACIDPeroxisome proliferator-activated receptor gammaEC 50 (nM)570N/AN/ADetails
(S)-3-(4-(2-Carbazol-9-Yl-Ethoxy)-Phenyl)-2-Ethoxy-Propionic AcidPeroxisome proliferator-activated receptor gammaEC 50 (nM)170N/AN/ADetails
FenofibratePeroxisome proliferator-activated receptor alphaEC 50 (nM)3210N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)4100N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)160N/AN/ADetails