Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.
Article Details
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Rittle KE, Barrow JC, Cutrona KJ, Glass KL, Krueger JA, Kuo LC, Lewis SD, Lucas BJ, McMasters DR, Morrissette MM, Nantermet PG, Newton CL, Sanders WM, Yan Y, Vacca JP, Selnick HG
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.
Bioorg Med Chem Lett. 2003 Oct 20;13(20):3477-82.
- PubMed ID
- 14505652 [ View in PubMed]
- Abstract
Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the alpha-thrombin-hirugen complex provides an explanation for these unanticipated results.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) D-phenylalanyl-N-(3-chlorobenzyl)-L-prolinamide Prothrombin Ki (nM) 250 N/A N/A Details D-phenylalanyl-N-benzyl-L-prolinamide Prothrombin Ki (nM) 4600 N/A N/A Details