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 thrombin with Ki values up to 11 nM.
Zega
A
A
Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia.
Trampus-Bakija
A
A
Fortuna
M
M
Stegnar
M
M
Tschopp
T B
TB
Steiner
B
B
Urleb
U
U
D000925:Anticoagulants / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D001777:Blood Coagulation; D004355:Drug Stability; D006801:Humans; D066298:In Vitro Techniques; D010314:Partial Thromboplastin Time; D011517:Prothrombin Time; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors*; D013918:Thrombin Time
D000925:Anticoagulants; D013917:Thrombin