Synthesis and SAR of thrombin inhibitors incorporating a novel 4-amino-morpholinone scaffold: Analysis of X-ray crystal structure of enzyme inhibitor complex

Journal of Medicinal Chemistry

Volumn 46, Issue 19, 2003, Pages 3985-4001

  Nilsson, Jonas W ^a   Kvarnström, Ingemar ^a   Musil, Djordje ^b   Nilsson, Ingemar ^b   Samulesson, Bertil ^c,d  

^a LINKÖPING UNIVERSITY   (Sweden)

^b ASTRAZENECA R AND D   (Sweden)

^c STOCKHOLM UNIVERSITY   (Sweden)

^d MEDIVIR AB   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMIDINOBENZYLAMINE; 4 AMINO 2 CARBOXYMETHYL 3 MORPHOLINONE; ARGININE; BENZYLAMINE DERIVATIVE; DEXTRO PHENYLALANYLPROLINE 4 AMIDINOBENZYLAMINE; DEXTRO PHENYLALANYLPROLYLARGININE; MALIC ACID; MORPHOLINE DERIVATIVE; N (4 AMIDINOBENZYL) [4 (2,5 DIMETHOXYBENZENESULFONYLAMINO) 3 OXOMORPHOLIN 2 YL]ACETAMIDE ACETATE; THROMBIN; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CRYSTAL STRUCTURE; DRUG POTENCY; DRUG SYNTHESIS; ENZYME INHIBITOR INTERACTION; ESTERIFICATION; PROTON NUCLEAR MAGNETIC RESONANCE; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; THROMBOEMBOLISM; X RAY CRYSTALLOGRAPHY;

AMINO ACID SEQUENCE; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, MOLECULAR; MORPHOLINES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THROMBIN;

EID: 0141567465     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0307990     Document Type: Article

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