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Bioorg Med Chem. 2012 Feb 15;20(4):1557-68. doi: 10.1016/j.bmc.2011.12.040. Epub 2011 Dec 27.

Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).

Author information

1
Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.

Abstract

Recent drug discovery programs targeting urokinase plasminogen activator (uPA) have resulted in nonpeptidic inhibitors consisting of amidine or guanidine functional groups attached to aromatic or heteroaromatic scaffolds. There is a general problem of poor oral bioavailability of these charged inhibitors. In this paper, we report the synthesis and evaluation of a series of naphthamide and naphthalene sulfonamides as uPA inhibitors containing non-basic groups as substitute for amidine or guanidine groups.

PMID:
22285569
DOI:
10.1016/j.bmc.2011.12.040
[Indexed for MEDLINE]

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