2. Academic Validation
  3. Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins

Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins

  • Bioorg Med Chem Lett. 2004 Oct 18;14(20):5227-32. doi: 10.1016/j.bmcl.2004.06.061.
Bart L De Corte 1,  William A Kinney,  Li Liu,  Shyamali Ghosh,  Livia Brunner,  William J Hoekstra,  Rosemary J Santulli,  Robert W Tuman,  Judith Baker,  Candace Burns,  Jef C Proost,  Brett A Tounge,  Bruce P Damiano,  Bruce E Maryanoff,  Dana L Johnson,  Robert A Galemmo Jr
Affiliations

Affiliation

  • 1 Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, Spring House, PA 19477-0776, USA. bdecorte@prdus.jnj.com
PMID: 15380233 DOI: 10.1016/j.bmcl.2004.06.061
Abstract

The synthesis and SAR of a new class of piperidine-based alphavbeta3/alphavbeta5 Integrin antagonists is described. Replacement of an amide bond in a prototype isonipecotamide by a C-C isostere, and adjustment of the spacer length between the carboxylic acid and basic moieties, led to low nanomolar antagonists of alphavbeta3 and/or alphavbeta5 integrins with excellent selectivity versus alpha(IIb)beta3.

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