1445902-03-3Relevant academic research and scientific papers
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists
Fauber, Benjamin P.,René, Olivier,De Leon Boenig, Gladys,Burton, Brenda,Deng, Yuzhong,Eidenschenk, Céline,Everett, Christine,Gobbi, Alberto,Hymowitz, Sarah G.,Johnson, Adam R.,La, Hank,Liimatta, Marya,Lockey, Peter,Norman, Maxine,Ouyang, Wenjun,Wang, Weiru,Wong, Harvey
, p. 3891 - 3897 (2014/09/17)
Using structure-based drug design principles, we identified opportunities to reduce the lipophilicity of our tertiary sulfonamide RORc inverse agonists. The new analogs possessed improved RORc cellular potencies with >77-fold selectivity for RORc over oth
