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

Bioorganic & Medicinal Chemistry Letters
Bart L De CorteRobert 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.

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Citations

Aug 13, 2011·Chemical Reviews·Vellaisamy SridharanJ Carlos Menéndez
Sep 26, 2017·Angewandte Chemie·Richard J D HatleyPauline T Lukey
May 21, 2008·The Journal of Organic Chemistry·Javier I Bardagí, Roberto A Rossi
Mar 18, 2017·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Jessica LohrkeAndrew W Stephens
Jul 1, 2018·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Chanwoo KimDae Hyuk Moon
Feb 27, 2014·Journal of Medicinal Chemistry·Helen M Sheldrake, Laurence H Patterson
Nov 15, 2005·Journal of Combinatorial Chemistry·Roland E Dolle

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