[4-(2H-1,2,3-Benzotriazol-2-yl)phenoxy]alkanoic Acids as Agonists of Peroxisome Proliferator-Activated Receptors (PPARs)
Anna Sparatore
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, I-20131 Milan (phone: +39 0250317554; fax: +39 0250317565)
Search for more papers by this authorCristina Godio
Dipartimento di Scienze Farmacologiche, Università di Milano, Via Balzaretti 9, I-20133 Milan
Search for more papers by this authorElena Perrino
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, I-20131 Milan (phone: +39 0250317554; fax: +39 0250317565)
Search for more papers by this authorSergio Romeo
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, I-20131 Milan (phone: +39 0250317554; fax: +39 0250317565)
Search for more papers by this authorBart Staels
U545 Inserm, Departement d'Atherosclerose, Institut Pasteur de Lille and Faculté de Pharmacie, Université de Lille 2, 1 rue du Prof. Calmette, F-59019 Lille Cedex
Search for more papers by this authorJean-Charles Fruchart
U545 Inserm, Departement d'Atherosclerose, Institut Pasteur de Lille and Faculté de Pharmacie, Université de Lille 2, 1 rue du Prof. Calmette, F-59019 Lille Cedex
Search for more papers by this authorMaurizio Crestani
Dipartimento di Scienze Farmacologiche, Università di Milano, Via Balzaretti 9, I-20133 Milan
Search for more papers by this authorAnna Sparatore
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, I-20131 Milan (phone: +39 0250317554; fax: +39 0250317565)
Search for more papers by this authorCristina Godio
Dipartimento di Scienze Farmacologiche, Università di Milano, Via Balzaretti 9, I-20133 Milan
Search for more papers by this authorElena Perrino
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, I-20131 Milan (phone: +39 0250317554; fax: +39 0250317565)
Search for more papers by this authorSergio Romeo
Istituto di Chimica Farmaceutica e Tossicologica, Università di Milano, Viale Abruzzi 42, I-20131 Milan (phone: +39 0250317554; fax: +39 0250317565)
Search for more papers by this authorBart Staels
U545 Inserm, Departement d'Atherosclerose, Institut Pasteur de Lille and Faculté de Pharmacie, Université de Lille 2, 1 rue du Prof. Calmette, F-59019 Lille Cedex
Search for more papers by this authorJean-Charles Fruchart
U545 Inserm, Departement d'Atherosclerose, Institut Pasteur de Lille and Faculté de Pharmacie, Université de Lille 2, 1 rue du Prof. Calmette, F-59019 Lille Cedex
Search for more papers by this authorMaurizio Crestani
Dipartimento di Scienze Farmacologiche, Università di Milano, Via Balzaretti 9, I-20133 Milan
Search for more papers by this authorAbstract
A series of [4-(2H-1,2,3-benzotriazol-2-yl)phenoxy]alkanoic acids has been synthesized and tested as agonists of Peroxisome Proliferator-Activated Receptor (PPAR) α, γ, and δ. Three compounds displayed 56 to 96% of maximal activity of the reference drug Wy-14643 on PPARα, and two of these, i.e., 1 and 5, exhibited also moderate activity on either PPARγ or δ with efficacy equal to 50% and 46% of that of rosiglitazone and GW 501516, respectively. Thus, compounds 1 and 5 represent interesting starting point for preparing novel agents for the treatment of dyslipidemia or of dyslipidemic type-2 diabetes.
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