The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.

Wayne L. Cody,Cuiman Cai,Annette Marian Doherty,Jeremy J. Edmunds,John X. He,Lakshmi S. Narasimhan,Janet S. Plummer,Stephen T. Rapundalo,J. Ronald Rubin,Chad A. Van Huis,Yves St-Denis,Peter D. Winocour,M. Arshad Siddiqui

The design of potent and selective inhibitors of thrombin utilizing a piperazinedione template: part 1.

1999

Wayne L. Cody
Cuiman Cai
Annette Marian Doherty
Jeremy J. Edmunds
John X. He
Lakshmi S. Narasimhan
Janet S. Plummer
Stephen T. Rapundalo
J. Ronald Rubin
Chad A. Van Huis
Yves St-Denis
Peter D. Winocour
M. Arshad Siddiqui

Utilizing X-ray crystallography and molecular modeling, highly potent and selective peptidomimetic thrombin inhibitors have been designed containing a rigid piperazinedione template. The synthesis and biological activity of these compounds will be described.

Keywords:

Piperazinedione
Chemical synthesis
Peptidomimetic
Thrombin
Enzyme inhibitor
Molecular model
Discovery and development of direct thrombin inhibitors
Biological activity
Stereochemistry
Organic chemistry
Biochemistry
Chemistry

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