Improved Ca(v)2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide

[Image: see text] We report the investigation of sulfonamide-derived Ca(v)2.2 inhibitors to address drug-metabolism liabilities with this lead class of analgesics. Modification of the benzamide substituent provided improvements in both potency and selectivity. However, we discovered that formation o...

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Detalhes bibliográficos
Main Authors: Shao, Pengcheng P., Ye, Feng, Chakravarty, Prasun K., Herrington, James B., Dai, Ge, Bugianesi, Randal M., Haedo, Rodolfo J., Swensen, Andrew M., Warren, Vivien A., Smith, McHardy M., Garcia, Maria L., McManus, Owen B., Lyons, Kathryn A., Li, Xiaohua, Green, Mitchell, Jochnowitz, Nina, McGowan, Erin, Mistry, Shruti, Sun, Shu-Yu, Abbadie, Catherine, Kaczorowski, Gregory J., Duffy, Joseph L.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2013
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4027232/
https://ncbi.nlm.nih.gov/pubmed/24900606
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml4002612
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