Synthesis, in vitro and in silico evaluation of L-tyrosine containing PPARα/γ dual agonists

被引：10
|
作者：
Kumar, Rakesh
Ramachandran, Uma
Khanna, Smriti
Bharatam, Prasad V.
Raichur, Suryaprakash
Chakrabarti, Ranjan
机构：
[1] NIPER, Dept Med Chem, SAS Nagar 160062, India
[2] NIPER, Dept Pharmaceut Technol, SAS Nagar 160062, India
[3] Dr Reddys Labs, Discovery Biol, Hyderabad 500050, Andhra Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 03期
关键词：
PPAR; dual agonists L-tyrosine; transactivation; molecular docking;
D O I：
10.1016/j.bmc.2006.06.063
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A novel series of L-tyrosine derivatives have been reported with potential PPAR alpha/gamma dual agonistic activity. In vitro cell based PPAR alpha/gamma transactivation studies have shown compound 4a and compound 4f to be the most potent PPAR gamma and PPAR alpha activators, respectively. Molecular docking studies performed on these series of compounds have complemented the experimental results and have led to interesting inferences. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1547 / 1555
页数：9
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