Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.

Article Details

Citation

Copy to clipboard

Ries UJ, Priepke HW, Hauel NH, Haaksma EE, Stassen JM, Wienen W, Nar H

Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2291-5.

PubMed ID

12824020 [ View in PubMed

]

Abstract

Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight (M(W): 335-391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
4-(5-BENZENESULFONYLAMINO-1-METHYL-1H-BENZOIMIDAZOL-2-YLMETHYL)-BENZAMIDINE	Prothrombin	IC 50 (nM)	1500	N/A	N/A	Details