194162-86-2Relevant academic research and scientific papers
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists
Sall, Daniel J.,Arfsten, Ann E.,Bastian, Jolie A.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Morin Jr., John M.,Rose, Jack W.,Scarborough, Robert M.,Smyth, Mark S.,Um, Suzane L.,Utterback, Barbara G.,Vasileff, Robert T.,Wikel, James H.,Wyss, Virginia L.,Jakubowski, Joseph A.
, p. 2843 - 2857 (2007/10/03)
The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists is described. The additional conformational restriction offered by the bicyclic nucleus results in 20-400-fold increases in potency compared to the freely flexible, acyclic benzamidine counterpart. The design, synthesis, structure-activity relationships (SAR), and in vitro activity of this novel class of GPIIb-IIIa antagonists are presented.
