Design and Synthesis of a Potent and Selective Triazolone-Based Peroxisome Proliferator-Activated Receptor α Agonist

A new series of hPPARα agonists containing a 2,4-dihydro-3H-1,2,4-triazol-3-one (triazolone) core is described leading to the discovery of 5 (LY518674), a highly potent and selective PPARα agonist.

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Veröffentlicht in:	Journal of medicinal chemistry 2003-11, Vol.46 (24), p.5121-5124
Hauptverfasser:	Xu, Yanping, Mayhugh, Daniel, Saeed, Ashraf, Wang, Xiaodong, Thompson, Richard C, Dominianni, Samuel J, Kauffman, Raymond F, Singh, Jaipal, Bean, James S, Bensch, William R, Barr, Robert J, Osborne, John, Montrose-Rafizadeh, Chahrzad, Zink, Richard W, Yumibe, Nathan P, Huang, Naijia, Luffer-Atlas, Debra, Rungta, Deepa, Maise, Dale E, Mantlo, Nathan B
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Apolipoprotein A-I - genetics Binding, Competitive Biological and medical sciences Biological Availability Cell Line Dogs Drug Design General and cellular metabolism. Vitamins Humans Medical sciences Mice Mice, Transgenic Miscellaneous Pharmacology. Drug treatments Propionates - chemical synthesis Propionates - chemistry Propionates - pharmacology Radioligand Assay Rats Receptors, Cytoplasmic and Nuclear - agonists Structure-Activity Relationship Transcription Factors - agonists Transcription Factors - metabolism Transfection Triazoles - chemical synthesis Triazoles - chemistry Triazoles - pharmacology
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Beschreibung
Zusammenfassung:	A new series of hPPARα agonists containing a 2,4-dihydro-3H-1,2,4-triazol-3-one (triazolone) core is described leading to the discovery of 5 (LY518674), a highly potent and selective PPARα agonist.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm034173l