title: Synthesis and evaluation of N-acetyl-L-tyrosine based compounds as PPARalpha selective activators.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
authors.forename: Rakesh
authors.initials: R
authors.lastname: Kumar
authors.forename: Uma
authors.initials: U
authors.lastname: Ramachandran
authors.forename: Suryaprakash
authors.initials: S
authors.lastname: Raichur
authors.forename: Ranjan
authors.initials: R
authors.lastname: Chakrabarti
authors.forename: Rahul
authors.initials: R
authors.lastname: Jain
mesh_terms: 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
chemical_list: D047493:PPAR alpha; D014443:Tyrosine; C025787:N-acetyltyrosine