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Updated: Aug 8, 2026

Modification and Functionalization of the Guanidine Group by Tailor-made Precursors
Published on: April 27, 2017
alpha(v)beta(3) Antagonists based on a central thiophene scaffold
A Peyman1, K Scheunemann, D W Will
1Aventis Pharma Deutschland GmbH, D-65926, Frankfurt, Germany. anusch.peyman@aventis.com
Abstract:
A series of novel, highly potent alpha(v)beta(3) 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 beta-amino acids were explored with respect to inhibition of alpha(v)beta(3) mediated cell adhesion and selectivity versus alpha(IIb)beta(3) binding. In addition, compound 19 was found to be active in the TPTX model of osteoporosis.
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