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Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics
M Li1, Z Lin, M E Johnson
1Center for Pharmaceutical Biotechnology and Department of Medicinal Chemistry & Pharmacognosy, University of Illinois at Chicago, 60607-7173, USA.
Bioorganic & Medicinal Chemistry Letters
|August 18, 1999
Abstract:
Based on the structure of the thrombin--NAPAP complex, phosphinic dipeptide mimetics were designed as novel thrombin inhibitors. Synthesis and evaluation of these inhibitors revealed a promising lead with an IC50 of 0.6 microM.