Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties

  • Bioorg Med Chem Lett. 2013 May 1;23(9):2560-5. doi: 10.1016/j.bmcl.2013.02.116.
Tetsuyoshi Matsufuji  1 ,  Mika Ikeda ,  Asuka Naito ,  Masakazu Hirouchi ,  Shoichi Kanda ,  Masanori Izumi ,  Jun Harada ,  Tsuyoshi Shinozuka
Affiliations
  • 1. Lead Discovery & Optimization Research Laboratories I, Daiichi Sankyo Co., Ltd, 1-2-58 Hiromachi, Tokyo 140-8710, Japan.
PMID: 23528296 DOI: 10.1016/j.bmcl.2013.02.116
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.

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