New 2-Aryloxy-3-phenyl-propanoic Acids As Peroxisome Proliferator-Activated Receptors alpha/gamma Dual Agonists with Improved Potency and Reduced Adverse Effects on skeletal muscle function (Articolo in rivista)

Type
Label
  • New 2-Aryloxy-3-phenyl-propanoic Acids As Peroxisome Proliferator-Activated Receptors alpha/gamma Dual Agonists with Improved Potency and Reduced Adverse Effects on skeletal muscle function (Articolo in rivista) (literal)
Anno
  • 2009-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1021/jm900941b (literal)
Alternative label
  • Giuseppe Fracchiolla (a), Antonio Laghezza (a), Luca Piemontese (a), Paolo Tortorella (a), Fernando Mazza (b,c), Roberta Montanari (a), Giorgio Pochetti (a), Antonio Lavecchia (d), Ettore Novellino (d), Sabata Pierno (e), Diana Conte Camerino (e) and Fulvio Loiodice (a) (2009)
    New 2-Aryloxy-3-phenyl-propanoic Acids As Peroxisome Proliferator-Activated Receptors alpha/gamma Dual Agonists with Improved Potency and Reduced Adverse Effects on skeletal muscle function
    in Journal of medicinal chemistry
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Giuseppe Fracchiolla (a), Antonio Laghezza (a), Luca Piemontese (a), Paolo Tortorella (a), Fernando Mazza (b,c), Roberta Montanari (a), Giorgio Pochetti (a), Antonio Lavecchia (d), Ettore Novellino (d), Sabata Pierno (e), Diana Conte Camerino (e) and Fulvio Loiodice (a) (literal)
Pagina inizio
  • 6382 (literal)
Pagina fine
  • 6393 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 52 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo
  • 20 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • a Dipartimento Farmaco-Chimico, Università degli Studi di Bari, via Orabona 4, 70126 Bari, Italy b Dipartimento di Scienze Della Salute, Università di L'Aquila, 67010 L'Aquila, Italy c Istituto di Cristallografia, Consiglio Nazionale Delle Ricerche, Monterotondo Stazione, Montelibretti, 00016 Roma, Italy d Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli Federico II, via Montesano 49, 80131 Napoli, Italy e Dipartimento Farmaco-Biologico, Università degli Studi di Bari, via Orabona 4, 70126 Bari, Italy (literal)
Titolo
  • New 2-Aryloxy-3-phenyl-propanoic Acids As Peroxisome Proliferator-Activated Receptors alpha/gamma Dual Agonists with Improved Potency and Reduced Adverse Effects on skeletal muscle function (literal)
Abstract
  • The preparation of a new series of 2-aryloxy-3-phenyl-propanoic acids, resulting from the introduction of a linker into the diphenyl system of the previously reported PPAR±/³ dual agonist 1, allowed the identification of new ligands with improved potency on PPAR± and unchanged activity on PPAR³. For the most interesting stereoisomers S-2 and S-4, X-ray studies in PPAR³ and docking experiments in PPAR± provided a molecular explanation for their different behavior as full and partial agonists of PPAR± and PPAR³, respectively. Due to the adverse effects provoked by hypolipidemic drugs on skeletal muscle function, we also investigated the blocking activity of S-2 and S-4 on skeletal muscle membrane chloride channel conductance and found that these ligands have a pharmacological profile more beneficial compared to fibrates currently used in therapy. (literal)
Prodotto di
Autore CNR

Incoming links:


Autore CNR di
Prodotto
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi
data.CNR.it