An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798).

@article{Stupple2011AnIS,
  title={An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-\{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl\}acetamide (PF-232798).},
  author={Paul A. Stupple and David V J Batchelor and Martin Corless and Patrick K Dorr and David G. Ellis and David R Fenwick and S{\'e}bastien R G Galan and R Morris Jones and Helen J. Mason and D. Stewart Middleton and Manos Perros and Francesca Perruccio and Michelle Y Platts and D C Pryde and Deborah Rodrigues and Nicholas N Smith and Peter T Stephenson and Robert Webster and Mike Westby and Anthony Wood},
  journal={Journal of medicinal chemistry},
  year={2011},
  volume={54 1},
  pages={67-77}
}
Preventing entry of HIV into human host cells has emerged as an attractive approach to controlling viral replication. Maraviroc 1 is an approved antagonist of the human CCR5 receptor which prevents the entry of HIV. Herein, we report the design and discovery of a series of imidazopiperidine CCR5 antagonists which retain the attractive antiviral profile and window over hERG activity of maraviroc 1, combined with improved absorption profiles in rat and dog. Furthermore, this series of compounds… CONTINUE READING
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