Novel 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles as PPARγ agonists

被引：22

作者：

Blanc-Delmas, Elodie

Lebegue, Nicolas

Wallez, Valerie

Leclerc, Veronique

Yous, Said

Carato, Pascal

Farce, Amaury

Bennejean, Caroline

Renard, Pierre

Caignard, Daniel-Henri

Audinot-Bouchez, Valerie

Chomarat, Pascale

Boutin, Jean

Hennuyer, Nathalie

Louche, Katie

Carmona, Maria Carmen

Staels, Bart

Penicaud, Luc

Casteilla, Louis

Lonchampt, Michel

Dacquet, Catherine

Chavatte, Philippe

Berthelot, Pascal

Lesieur, Daniel

机构：

[1] Fac Sci Pharmaceut & Biol Lille, Chim Therapeut Lab, EA 1043, F-59006 Lille, France

[2] Inst Rech Int Servier, F-92415 Courbevoie, France

[3] Inst Rech Servier, F-92150 Suresnes, France

[4] Inst Rech Servier, F-78190 Croissy Sur Seine, France

[5] Inst Rech Servier, Div Pharmacol Mol & Cellulaire, F-78000 Versailles, France

[6] Inst Pasteur, INSERM, Dept Atherosclerose, F-59019 Lille, France

[7] CHU Rangueil, Univ Toulouse 3, Lab Neurobiol Plast Tissul & Metab, UMR 5018, F-31054 Toulouse, France

[8] Inst Rech Servier, Div Rech Maladies Metab, F-92150 Suresnes, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 22期

关键词：

diabetes; PPAR gamma; benzothiazolone; benzoxazolone; 1,3-dicarbonyl derivative; molecular modeling;

D O I：

10.1016/j.bmc.2006.07.029

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

A series of 1,3-dicarbonyl compounds having 2(3H)-benzazolonic heterocycles has been synthesized and tested for PPAR gamma agonist activity. SAR were developed and revealed that 6-acyl-2(3H)-benzothiazolone derivatives with 1,3-dicarbonyl group were the most potent. IP administration of compound 22 exhibited comparable levels of glucose and triglyceride correction to PO administration of rosiglitazone in the oblob mouse studies. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：7377 / 7391

页数：15

共 36 条

[1]

A NOVEL-APPROACH TO DUAL-ACTING THROMBOXANE RECEPTOR ANTAGONIST AND SYNTHASE INHIBITORS BASED ON THE LINK OF 1,3-DIOXANE-THROMBOXANE RECEPTOR ANTAGONISTS AND 1,3-DIOXANE-THROMBOXANE SYNTHASE INHIBITORS [J].