Synthesis, in vitro and in silico evaluation of l-tyrosine containing PPARalpha/gamma dual agonists.
A novel series of l-tyrosine derivatives have been reported with potential PPARalpha/gamma dual agonistic activity. In vitro cell based PPARalpha/gamma transactivation studies have shown compound 4a and compound 4f to be the most potent PPARgamma and PPARalpha activators, respectively. Molecular docking studies performed on these series of compounds have complemented the experimental results and have led to interesting inferences.
Kumar
Rakesh
R
Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S. A. S. Nagar 160 062, India.
Ramachandran
Uma
U
Khanna
Smriti
S
Bharatam
Prasad V
PV
Raichur
Suryaprakash
S
Chakrabarti
Ranjan
R
D019295:Computational Biology; D006801:Humans; D066298:In Vitro Techniques; D008958:Models, Molecular; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D013329:Structure-Activity Relationship; D014443:Tyrosine / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D047493:PPAR alpha; D047495:PPAR gamma; D014443:Tyrosine