188200-08-0Relevant academic research and scientific papers
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2-P3 bicyclic lactam moiety
Tamura, Susan Y.,Goldman, Erick A.,Brunck, Terence K.,Ripka, William C.,Semple, J. Edward
, p. 331 - 336 (2007/10/03)
Based on molecular modeling and judicious combination of the salient topographic features of the recently discovered P3-lactam derivative 1 with the P2-prolyl derivatives 2a,b, the novel thrombin inhibitor 3a was designed. Inhibitor 3a incorporates a fused bicyclic lactam as a novel type of P2-P3 dipeptide surrogate. The synthesis and biological activity of this potent serine protease inhibitor is presented.
