Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.

@article{Herbert2010SynthesisAS,
  title={Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.},
  author={Mark R. Herbert and Dana L Siegel and Lena M. Staszewski and Charmagne S Cayanan and Urmi Banerjee and Sangeeta Dhamija and Jennifer J. Anderson and Amy Fan and Li Wang and Peter J. Rix and Andrew K. Shiau and Tadimeti S. Rao and Stewart A. Noble and Richard A. Heyman and Eric D. Bischoff and Mausumee Guha and Ayman Kabakibi and Anthony B Pinkerton},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 19},
  pages={5718-21}
}
Optimization of a screening hit from uHTS led to the discovery of TGR5 agonist 32, which was shown to have activity in a rodent model for diabetes.