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Bioorg Med Chem Lett. 2001 Aug 6;11(15):2011-5.

alpha(v)beta(3) Antagonists based on a central thiophene scaffold.

Author information

1
Aventis 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.

PMID:
11454469
DOI:
10.1016/s0960-894x(01)00357-2
[Indexed for MEDLINE]

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