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Bioorg Med Chem Lett. 2005 Sep 15;15(18):4053-6.

Influence of acid surrogates toward potency of VLA-4 antagonist.

Author information

1
Department of Chemistry, Merck Research Laboratories, 3535 General Atomics Court, San Diego, CA 92121, USA. shankar_venkatraman@merck.com

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.

PMID:
16039122
DOI:
10.1016/j.bmcl.2005.06.034
[Indexed for MEDLINE]

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