基于N-乙酰-L-酪氨酸的化合物作为PPARα选择性激活剂的合成与评价
Synthesis and evaluation of N-acetyl-L-tyrosine based compounds as PPARalpha selective activators.
作者信息
Kumar Rakesh, Ramachandran Uma, Raichur Suryaprakash, Chakrabarti Ranjan, Jain Rahul
机构信息
Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Punjab 160 062, India.
出版信息
Eur J Med Chem. 2007 Apr;42(4):503-10. doi: 10.1016/j.ejmech.2006.11.005. Epub 2006 Nov 19.
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.
肥胖个体中2型糖尿病的发展与非脂肪组织中的脂质积累有关。合成了一系列N-乙酰-L-酪氨酸衍生物，并对其进行了PPAR反式激活评估。发现化合物4d和4f与PPARγ相比显示出更好的PPARα反式激活作用。进行了分子对接分析以研究它们与PPARα活性位点的重要相互作用。
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