497159-99-6Relevant academic research and scientific papers
IMIDAZOLE DERIVATIVES USED AS TAFIA INHIBITORS
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Page/Page column 50-51, (2010/02/14)
The invention relates to compounds of formula (I), which are inhibitors of the activated thrombin-activatable fibrinolysis inhibitor. The compounds of formula (I) are suited for producing medicaments for the prevention and treatment of diseases accompanied by thromboses, embolisms, hypercoagulability or fibrotic changes.
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P′1 group
Nantermet, Philippe G.,Barrow, James C.,Lindsley, Stacey R.,Young, Marybeth,Mao, Shi-Shan,Carroll, Steven,Bailey, Carolyn,Bosserman, Michele,Colussi, Dennis,McMasters, Daniel R.,Vacca, Joseph P.,Selnick, Harold G.
, p. 2141 - 2145 (2007/10/03)
Structural modifications of the aminopyridine P1 ′ group of imidazole acetic acid based TAFIa inhibitors led to the discovery of the aminocyclopentyl analog 28, a 1nM TAFIa inhibitor with CLT50 functional activity of 14nM but without selectivity against CPB. While not as active, aminobutyl derivative 27 provided an improved 6.7-fold selectivity for TAFIa versus CPB.
Synthesis and Evaluation of Imidazole Acetic Acid Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor as Novel Antithrombotics
Barrow, James C.,Nantermet, Philippe G.,Stauffer, Shaun R.,Ngo, Phung L.,Steinbeiser, Melissa A.,Mao, Shi-Shan,Carroll, Steven S.,Bailey, Carolyn,Colussi, Dennis,Bosserman, Michelle,Burlein, Christine,Cook, Jacquelynn J.,Sitko, Gary,Tiller, Philip R.,Miller-Stein, Cynthia M.,Rose, Mark,McMasters, Daniel R.,Vacca, Joseph P.,Selnick, Harold G.
, p. 5294 - 5297 (2007/10/03)
Thrombin-activatable fibrinolysis inhibitor (TAFI) is an important regulator of fibrinolysis, and inhibitors of this enzyme have potential use in antithrombotic and thrombolytic therapy. Appropriately substituted imidazole acetic acids such as 10j were fo
