Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.

@article{Pizzonero2014DiscoveryAO,
  title={Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.},
  author={Mathieu Pizzonero and Sonia Dupont and Marielle Babel and St{\'e}phane Beaumont and Natacha Bienvenu and Roland Blanqu{\'e} and La{\"e}titia Cherel and Thierry Christophe and Benedetta Crescenzi and Elsa de Lemos and Philippe Delerive and Pierre D{\'e}prez and Steve De Vos and Fatoumata Djata and Stephen D. Fletcher and Sabrina Kopiejewski and Christelle L'Ebraly and J M Lefrançois and St{\'e}phanie Lavazais and Murielle Manioc and Luc Nelles and Line Oste and D. Polancec and Vanessa Qu{\'e}n{\'e}hen and Floril{\`e}ne Soulas and Nicolas Triballeau and Ellen M van der Aar and Nick Vandeghinste and Emanuelle Wakselman and Reginald Brys and Laurent Sani{\`e}re},
  journal={Journal of medicinal chemistry},
  year={2014},
  volume={57 23},
  pages={10044-57}
}
FFA2, also called GPR43, is a G-protein coupled receptor for short chain fatty acids which is involved in the mediation of inflammatory responses. A class of azetidines was developed as potent FFA2 antagonists. Multiparametric optimization of early hits with moderate potency and suboptimal ADME properties led to the identification of several compounds with nanomolar potency on the receptor combined with excellent pharmacokinetic (PK) parameters. The most advanced compound, 4-[[(R)-1-(benzo[b… CONTINUE READING
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