| Literature DB >> 20022493 |
Thomas S Reger1, Jasmine Zunic, Nicholas Stock, Bowei Wang, Nicholas D Smith, Benito Munoz, Mitchell D Green, Michael F Gardner, Joyce P James, Weichao Chen, Kenneth Alves, Qian Si, Kelly M Treonze, Russell B Lingham, Richard A Mumford.
Abstract
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. Copyright (c) 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 20022493 DOI： 10.1016/j.bmcl.2009.12.009
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823