Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 6, 2011, Pages 1582-1587

  Young, Robert J ^a   Adams, Carl ^a   Blows, Mike ^a   Brown, David ^a   Burns Kurtis, Cynthia L ^b   Chan, Chuen ^a   Chaudry, Laiq ^a   Convery, Máire A ^a   Davies, David E ^a   Exall, Anne M ^a   Foster, Graham ^a   Harling, John D ^a   Hortense, Eric ^a   Irvine, Stephanie ^a   Irving, Wendy R ^a   Jackson, Steve ^a   Kleanthous, Savvas ^a   Pateman, Anthony J ^a   Patikis, Angela N ^a   Roethka, Theresa J ^b   Senger, Stefan ^a   Stelman, Gary J ^b   Toomey, John R ^b   West, Robert I ^a   Whittaker, Caroline ^a   Zhou, Ping ^a   Watson, Nigel S ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Factor Xa; Oral inhibitors; P450 inhibition; Property based design; Structure based design

Indexed keywords

AMINOINDANE; BLOOD CLOTTING FACTOR 10A INHIBITOR; CYTOCHROME P450; INDAN DERIVATIVE; PHENYLPYRROLIDINE DERIVATIVE; PYRROLIDINE DERIVATIVE; SULFONAMIDOPYRROLIDIN 2 ONE DERIVATIVE; UNCLASSIFIED DRUG;

ANTICOAGULATION; ARTICLE; CHEMICAL MODIFICATION; CRYSTAL STRUCTURE; DOSE TIME EFFECT RELATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HYDROPHOBICITY; MOLECULAR DOCKING; NONHUMAN; PHYSICAL CHEMISTRY; REACTION ANALYSIS; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION;

DRUG DESIGN; FACTOR XA; MODELS, MOLECULAR; PYRROLIDINES; SERINE PROTEINASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79952362136     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.01.131     Document Type: Article

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