Sulfonamidopyrrolidinone factor Xa inhibitors: Potency and selectivity enhancements via P-1 and P-4 optimization

Journal of Medicinal Chemistry

Volumn 42, Issue 18, 1999, Pages 3572-3587

  Choi Sledeski, Yong Mi ^a   McGarry, Daniel G ^a   Green, Daniel M ^a,b   Mason, Helen J ^a,c   Becker, Michael R ^a   Davis, Roderick S ^a   Ewing, William R ^a   Dankulich, William P ^a   Manetta, Vincent E ^a   Morris, Robert L ^a   Spada, Alfred P ^a   Cheney, Daniel L ^a,c   Brown, Karen D ^a   Colussi, Dennis J ^a   Valeria, Chu ^a   Heran, Christopher L ^a   Morgan, Suzanne R ^a   Bentley, Ross G ^a   Leadley, Robert J ^a   Maignan, Sebastien ^a   Guilloteau, Jean Pierre ^a   Dunwiddie, Christopher T ^a,d   Pauls, Henry W ^a   more..

^a Depts Cardiovasc Drug Discov/N   (United States)

^b WYETH AYERST RESEARCH   (United States)

^c BRISTOL MYERS SQUIBB   (United States)

^d ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 PYRROLIDONE DERIVATIVE; 4 HYDROXY 3 [2 OXO 3 (5 PYRIDIN 3 YLTHIOPHENE 2 YLSULFONYLAMINO)PYRROLIDIN 1 YLMETHYL)BENZAMIDINE TRIFLUOROACETATE; BLOOD CLOTTING FACTOR 10A INHIBITOR; RPR 130737; UNCLASSIFIED DRUG;

ARTICLE; BLOOD CLOTTING; DRUG POTENCY; ENZYME ACTIVITY; HYDROLYSIS; MOLECULAR MODEL; PARTIAL THROMBOPLASTIN TIME; PROTEIN DEGRADATION; THROMBOSIS; X RAY CRYSTALLOGRAPHY;

AMIDINES; ANIMALS; ANTICOAGULANTS; BINDING SITES; FACTOR XA; HUMANS; MODELS, MOLECULAR; PROTEIN BINDING; PYRROLIDINONES; RATS; RATS, SPRAGUE-DAWLEY; SERINE PROTEINASE INHIBITORS; SULFONAMIDES; SULFONES; THROMBOSIS;

EID: 0033539030     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm990041+     Document Type: Article

References (45)

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