Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin.

@article{Durgam2005SynthesisSR,
  title={Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin.},
  author={Gangadhar G. Durgam and Tamas Virag and Michelle Davidson Walker and Ryoko Tsukahara and Satoshi Yasuda and K{\'a}roly Liliom and Laurens A. van Meeteren and Wouter H Moolenaar and Nicole G Wilke and Wolfgang Siess and Gabor J Tigyi and Duane D. Miller},
  journal={Journal of medicinal chemistry},
  year={2005},
  volume={48 15},
  pages={
          4919-30
        }
}
We previously reported that fatty alcohol phosphates (FAP) represent a minimal pharmacophore required to interact with lysophosphatidic acid (LPA) receptors. To improve the activity of the first-generation saturated FAP series, a structure-activity relationship (SAR) study was carried out that includes modifications to the headgroup and alkyl side chain of the FAP pharmacophore. A series of unsaturated (C(10)-C(18)) FAP, headgroup-modified hydrolytically stable saturated (C(10)-C(18)) alkyl… CONTINUE READING
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