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Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 May 01; Vol. 23 (9), pp. 2560-5. Date of Electronic Publication: 2013 Mar 07. - Publication Year :
- 2013
-
Abstract
- 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.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Fatty Acid Transport Proteins metabolism
Half-Life
Humans
Liver metabolism
Mice
Muscle, Skeletal metabolism
Piperazines chemical synthesis
Piperazines pharmacokinetics
Protein Binding
Structure-Activity Relationship
Triglycerides metabolism
Fatty Acid Transport Proteins antagonists & inhibitors
Piperazines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 23528296
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.02.116