| Literature DB >> 15380233 |
Bart L De Corte1, 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.
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.Entities:
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Year: 2004 PMID： 15380233 DOI： 10.1016/j.bmcl.2004.06.061
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823