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Bioorg Med Chem Lett. 2002 Feb 25;12(4):611-4.

The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. linus_lin@merck.com

Erratum in

  • Bioorg Med Chem Lett. 2002 Jun 17;12(12):1695.

Abstract

Acylated beta-amino acids are described as potent, specific and orally bioavailable antagonists of VLA-4. The initial lead was identified from a combinatorial library. Subsequent optimization using a traditional medicinal chemistry approach led to significant improvement in potency (up to 8-fold) while maintaining good pharmacokinetic properties.

PMID:
11844683
DOI:
10.1016/s0960-894x(01)00818-6
[Indexed for MEDLINE]

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