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  • Title: Design, synthesis and molecular modelling of 1-amidinopiperidine thrombin inhibitors.
    Author: Smolnikar I, Perdih A, Stegnar M, Prezelj A, Solmajer T, Urleb U, Obreza A.
    Journal: Pharmazie; 2007 Apr; 62(4):243-54. PubMed ID: 17484277.
    Abstract:
    Design, synthesis and biochemical evaluation of a series of novel non-covalent thrombin inhibitors with a 1-amidinopiperidine moiety are presented. Replacement of the planar benzamidine group in azaphenylalanine derivatives with 1-amidinopiperidine resulted in lower activity but higher selectivity for this type of compounds. The binding conformation of inhibitors in the active site of thrombin was revealed by molecular modelling studies.
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