Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.

@article{Brown2010TriazoleOA,
  title={Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.},
  author={Alan D. G. Brown and Timothy B. Brown and Andrew Calabrese and Dave L. Ellis and Nicholas Puhalo and Michael J Ralph and Lesa Watson},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 2},
  pages={516-20}
}
A series of aryloxyazetidines, aryloxypyrrolidines and aryloxypiperidines were designed based on structural overlap with previously reported arylpyrazine Oxytocin antagonists. Similarly high levels of Oxytocin antagonism were achievable in these new series. Several aryloxyazetidines also showed high levels of selectivity, with one compound, 25, displaying promising in vivo pharmacokinetics and significantly improved aqueous solubility over related compounds containing a biaryl substituent. 

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