Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics.

Adang, Anton E P; de Man, Adrianus P A; Vogel, Gerard M T; Grootenhuis, Peter D J; Smit, Martin J; Peters, Co A M; Visser, Arie; Rewinkel, Jos B M; van Dinther, Theo; Lucas, Hans; Kelder, Jan; van Aelst, Sjoerd; Meuleman, Dick G; van Boeckel, Constant A A

Adang, Anton E P; de Man, Adrianus P A; Vogel, Gerard M T; Grootenhuis, Peter D J; Smit, Martin J; Peters, Co A M; Visser, Arie; Rewinkel, Jos B M; van Dinther, Theo; Lucas, Hans; Kelder, Jan; van Aelst, Sjoerd; Meuleman, Dick G; van Boeckel, Constant A A.

Affiliation

Adang AE; Research and Development, Lead Discovery Unit Chemistry Group, NV Organon. ton.adang@organon.com

J Med Chem ; 45(20): 4419-32, 2002 Sep 26.

Article in En | MEDLINE | ID: mdl-12238922

Subject(s)

Enzyme Inhibitors/chemical synthesis; Fibrinolytic Agents/chemical synthesis; Oligopeptides/chemical synthesis; Thrombin/antagonists & inhibitors; Administration, Oral; Animals; Aorta; Biological Availability; Biological Transport, Active; Caco-2 Cells; Crystallography, X-Ray; Dogs; Dose-Response Relationship, Drug; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology; Fibrinolytic Agents/chemistry; Fibrinolytic Agents/pharmacology; Half-Life; Humans; In Vitro Techniques; Models, Molecular; Oligopeptides/chemistry; Oligopeptides/pharmacology; Rats; Structure-Activity Relationship; Thrombosis/prevention & control

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Collection: 01-internacional Database: MEDLINE Main subject: Oligopeptides / Thrombin / Enzyme Inhibitors / Fibrinolytic Agents Limits: Animals / Humans Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2002 Type: Article

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