Author/Authors :
Shankar Venkatraman، نويسنده , , Jongwon Lim، نويسنده , , Merryl Cramer، نويسنده , , Michael F. Gardner، نويسنده , , Joyce James، نويسنده , , Kenneth Alves، نويسنده , , Russell B. Lingham، نويسنده , , Richard A. Mumford، نويسنده , , Benito Munoz، نويسنده ,
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.
