Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties
2013
Matsufuji, Tetsuyoshi | Ikeda, Mika | Naito, Asuka | Hirouchi, Masakazu | Kanda, Shoichi | Izumi, Masanori | Harada, Jun | Shinozuka, Tsuyoshi
The discovery and optimization of a novel series of FATP1 inhibitors are described. Through the derivatization process, arylpiperazine derivatives 5k and 12a were identified as possessing potent in vitro activity against human and mouse FATP1s as well as excellent pharmacokinetic properties. In vivo evaluation of triglyceride accumulation in the liver, white gastrocnemius muscle and soleus is also described.
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书目信息
Bioorganic & medicinal chemistry letters
卷
23
期
9
页码
2560
- 2565
ISSN
0960-894X
出版者
Elsevier Ltd
其它主题
Derivatization; In vivo studies
语言
英语
类型
Journal Article; Text
2024-02-28
MODS