Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
A new series of hPPARalpha 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 PPARalpha agonist.
Xu
Yanping
Y
Division of Eli Lilly & Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
Mayhugh
Daniel
D
Saeed
Ashraf
A
Wang
Xiaodong
X
Thompson
Richard C
RC
Dominianni
Samuel J
SJ
Kauffman
Raymond F
RF
Singh
Jaipal
J
Bean
James S
JS
Bensch
William R
WR
Barr
Robert J
RJ
Osborne
John
J
Montrose-Rafizadeh
Chahrzad
C
Zink
Richard W
RW
Yumibe
Nathan P
NP
Huang
Naijia
N
Luffer-Atlas
Debra
D
Rungta
Deepa
D
Maise
Dale E
DE
Mantlo
Nathan B
NB
D000284:Administration, Oral; D000818:Animals; D016632:Apolipoprotein A-I / Q000235:genetics; D001667:Binding, Competitive; D001682:Biological Availability; D002460:Cell Line; D004285:Dogs; D015195:Drug Design; D006801:Humans; D051379:Mice; D008822:Mice, Transgenic; D011422:Propionates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000819:agonists* / Q000378:metabolism; D014162:Transfection; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D016632:Apolipoprotein A-I; C479889:LY 518674; D011422:Propionates; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors; D014230:Triazoles