Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1378121 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
Abstract
A series of VLA-4 antagonist were synthesized wherein carboxylic acid was replaced by various acid surrogates. The effect of these acid surrogates toward potency was evaluated in a binding assay. A number of acid surrogates were potent antagonist of VLA-4, albeit significantly less potent than the corresponding carboxylic acid. Heterocyclic acid surrogate, oxadiazolidinone 3, demonstrated an improved pharmacokinetic property when dosed intravenously.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Shankar Venkatraman, Jongwon Lim, Merryl Cramer, Michael F. Gardner, Joyce James, Kenneth Alves, Russell B. Lingham, Richard A. Mumford, Benito Munoz,