179524-07-3Relevant academic research and scientific papers
Aromatic heterocyclic derivatives as enzyme inhibitors
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Page column 66-67, (2010/02/04)
The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
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.
