Identification of unique VLA-4 antagonists from a combinatorial library

  • Bioorg Med Chem Lett. 2002 Feb 25;12(4):685-8. doi: 10.1016/s0960-894x(01)00833-2.
Stephen E de Laszlo  1 ,  Bing Li ,  Ermengilda McCauley ,  Gail Van Riper ,  William K Hagmann
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
PMID: 11844701 DOI: 10.1016/s0960-894x(01)00833-2
Abstract

A combinatorial library of 28 pools of 180 compounds (345 diastereomers) was designed and prepared in support of the delineation of the SAR of two prototypical VLA-4 antagonists. Deconvolution of the active pools led to the identification of three novel series of VLA-4 antagonists with low nanomolar potencies.