Author/Authors :
Anusch Peyman، نويسنده , , Karl-Heinz Scheunemann، نويسنده , , David W. Will، نويسنده , , Jochen Knolle، نويسنده , , Volkmar Wehner، نويسنده , , Gerhard Breipohl، نويسنده , , Hans Ulrich Stilz، نويسنده , , Denis Carniato، نويسنده , , Jean-Marie Ruxer، نويسنده , , Jean-Francois Gourvest، نويسنده , , Marielle Auberval، نويسنده , , Bernard Doucet، نويسنده , , Roland Baron، نويسنده , , Martine Gaillard، نويسنده , , Thomas R. Gadek، نويسنده , , Sarah Bodary، نويسنده ,
Abstract :
A series of novel, highly potent αvβ3 antagonists based on a thiophene scaffold and containing an acylguanidine as an Arg-mimetic is described. A number of structural features, such as cyclic versus open guanidine and a variety of lipophilic side chains, carbamates, sulfonamides and β-amino acids were explored with respect to inhibition of αvβ3 mediated cell adhesion and selectivity versus αIIbβ3 binding. In addition, compound 19 was found to be active in the TPTX model of osteoporosis.
