1217275-18-7Relevant articles and documents
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists
Reger, Thomas S.,Zunic, Jasmine,Stock, Nicholas,Wang, Bowei,Smith, Nicholas D.,Munoz, Benito,Green, Mitchell D.,Gardner, Michael F.,James, Joyce P.,Chen, Weichao,Alves, Kenneth,Si, Qian,Treonze, Kelly M.,Lingham, Russell B.,Mumford, Richard A.
scheme or table, p. 1173 - 1176 (2010/06/15)
A variety of N-linked tertiary amines and heteroarylamines were examined at the 4-position of sulfonylated proline dipeptides in order to improve VLA-4 receptor off-rates and overcome the issue of CYP3A4 time-dependent inhibition of ester prodrugs. A tight-binding inhibitor 5j with a long off-rate provided sustained receptor occupancy despite poor oral pharmacokinetics.
