Novel thrombin inhibitors with azaphenylalanine scaffold

In this paper the synthesis and antithrombotic activity of a series of novel thrombin inhibitors with azaphenylalanine scaffold are described. By systematic structural modifications for this series we have identified optimal groups for achieving nanomolar potency, that led to potent inhibitors of th...

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Bibliographic Details
Published in:	Pharmazie Vol. 56; no. 9; p. 683
Main Authors:	Zega, A, Trampus-Bakija, A, Fortuna, M, Stegnar, M, Tschopp, T B, Steiner, B, Urleb, U
Format:	Journal Article
Language:	English
Published:	Germany 01-09-2001
Subjects:	Anticoagulants - chemical synthesis Anticoagulants - pharmacokinetics Anticoagulants - pharmacology Blood Coagulation Drug Stability Humans In Vitro Techniques Partial Thromboplastin Time Prothrombin Time Spectrophotometry, Ultraviolet Structure-Activity Relationship Thrombin - antagonists & inhibitors Thrombin Time
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Summary:	In this paper the synthesis and antithrombotic activity of a series of novel thrombin inhibitors with azaphenylalanine scaffold are described. By systematic structural modifications for this series we have identified optimal groups for achieving nanomolar potency, that led to potent inhibitors of thrombin with Ki values up to 11 nM.
ISSN:	0031-7144