Synthesis and evaluation of N-acetyl-L-tyrosine based compounds as PPARalpha selective activators.
The development of type 2 diabetes in obese individuals is linked to lipid accumulation in non-adipose tissues. A series of N-acetyl-L-tyrosine derivatives were synthesized and evaluated for PPAR transactivation. Compounds 4d and 4f were found to show better PPARalpha transactivation as compared to PPARgamma. Molecular docking analysis was carried out to study their important interactions with the active site of PPARalpha.
Kumar
Rakesh
R
Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
Ramachandran
Uma
U
Raichur
Suryaprakash
S
Chakrabarti
Ranjan
R
Jain
Rahul
R
D001665:Binding Sites / Q000187:drug effects; D002460:Cell Line; D003198:Computer Simulation; D004353:Drug Evaluation, Preclinical; D008954:Models, Biological; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D010957:Plasmids / Q000235:genetics; D015533:Transcriptional Activation / Q000187:drug effects; D014162:Transfection; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D047493:PPAR alpha; D014443:Tyrosine; C025787:N-acetyltyrosine