Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.

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Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.

PubMed ID

15582418 [ View in PubMed

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Abstract

A series of non-amide-linked 6-substituted-2-naphthamidine urokinase plasminogen activator (uPA) inhibitors are described. These compounds possess excellent binding activities and selectivities with significantly improved pharmacokinetic profiles versus previously described amide-linked inhibitors.

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
Trans-6-(2-Phenylcyclopropyl)-Naphthalene-2-Carboxamidine	Urokinase-type plasminogen activator	Ki (nM)	1310	N/A	N/A	Details