Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.

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Caijo F, Mosset P, Gree R, Audinot-Bouchez V, Boutin J, Renard P, Caignard DH, Dacquet C

Synthesis of new carbo- and heterocyclic analogues of 8-HETE and evaluation of their activity towards the PPARs.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4421-6.

PubMed ID

16137885 [ View in PubMed

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Abstract

A new class of dual PPARs alpha and gamma agonists was developed. These compounds are structural analogues of the arachidonic acid metabolite, the 8-(S)-HETE. A versatile strategy has been introduced to prepare the target molecules having different carbo- and heterocyclic cores and to modulate the unsaturations on the side chains. Their affinity towards the PPARs alpha and gamma receptors is reported, together with their transactivation percentage. Most of these derivatives have a good activity as dual agonists but the quinoline-derived products appear as the most promising compounds.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rosiglitazone	Peroxisome proliferator-activated receptor alpha	EC 50 (nM)	>10000	N/A	N/A	Details
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	Ki (nM)	8	N/A	N/A	Details
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	4	N/A	N/A	Details