Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).
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Venkatraj M, Messagie J, Joossens J, Lambeir AM, Haemers A, Van der Veken P, Augustyns K
Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).
Bioorg Med Chem. 2012 Feb 15;20(4):1557-68. doi: 10.1016/j.bmc.2011.12.040. Epub 2011 Dec 27.
- PubMed ID
- 22285569 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) 6-(N-Phenylcarbamyl)-2-Naphthalenecarboxamidine Urokinase-type plasminogen activator Ki (nM) 631 N/A N/A Details 6-(N-Phenylcarbamyl)-2-Naphthalenecarboxamidine Urokinase-type plasminogen activator IC 50 (nM) 13000 N/A N/A Details 6-(N-Phenylcarbamyl)-2-Naphthalenecarboxamidine Urokinase-type plasminogen activator Ki (nM) 1900 N/A N/A Details 6-[N-(4-(Aminomethyl)Phenyl)Carbamyl]-2-Naphthalenecarboxamidine Urokinase-type plasminogen activator Ki (nM) 40 N/A N/A Details 6-[N-(4-(Aminomethyl)Phenyl)Carbamyl]-2-Naphthalenecarboxamidine Urokinase-type plasminogen activator IC 50 (nM) 1200 N/A N/A Details