Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.
A novel series of potent dual agonists of PPARalpha and PPARgamma, the alkoxybenzylglycines, was identified and explored using a solution-phase library approach. The synthesis and structure-activity relationships of this series of dual PPARalpha/gamma agonists are described.
Devasthale
Pratik V
PV
Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. pratik.devasthale@bms.com
Chen
Sean
S
Jeon
Yoon
Y
Qu
Fucheng
F
Ryono
Denis E
DE
Wang
Wei
W
Zhang
Hao
H
Cheng
Lin
L
Farrelly
Dennis
D
Golla
Rajasree
R
Grover
Gary
G
Ma
Zhengping
Z
Moore
Lisa
L
Seethala
Ramakrishna
R
Sun
Wei
W
Doweyko
Arthur M
AM
Chandrasena
Gamini
G
Sleph
Paul
P
Hariharan
Narayanan
N
Cheng
Peter T W
PT
D000596:Amino Acids / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D005998:Glycine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008815:Mice, Inbred Strains; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D013329:Structure-Activity Relationship
D000596:Amino Acids; D001786:Blood Glucose; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D047493:PPAR alpha; D047495:PPAR gamma; D005998:Glycine