Discovery of diarylurea P2Y1 antagonists with improved aqueous solubility

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 11, 2013, Pages 3239-3243

  Wang, Tammy C ^a   Qiao, Jennifer X ^a   Clark, Charles G ^a   Jua, Ji ^a   Price, Laura A ^a   Wu, Qimin ^a   Chang, Ming ^a   Zheng, Joanna ^a   Huang, Christine S ^a   Everlof, Gerry ^a   Schumacher, William A ^a   Wong, Pancras C ^a   Seiffert, Dietmar A ^a   Stewart, Anne B ^a   Bostwick, Jeffrey S ^a   Crain, Earl J ^a   Watson, Carol A ^a   Rehfuss, Robert ^a   Wexler, Ruth R ^a   Lam, Patrick Y S ^a,b  

^a BRISTOL MYERS SQUIBB   (United States)

^b Lam Drug Discovery Consulting LLC   (United States)

Author keywords

Aqueous solubility; Diarylurea; In vivo efficacy bleeding model; P2Y1 antagonists; Structure activity relationship (SAR)

Indexed keywords

ADRENALIN; CLOPIDOGREL; DIARYLUREA; PURINE ANTAGONIST; PURINERGIC P2Y1 RECEPTOR; THROMBIN RECEPTOR ACTIVATING PEPTIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; BLEEDING TIME; CONTROLLED STUDY; DEMETHYLATION; DRUG CLEARANCE; DRUG DEVELOPMENT; DRUG EFFICACY; DRUG MEGADOSE; DRUG POTENCY; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; EX VIVO STUDY; HUMAN; HUMAN CELL; HYDROXYLATION; HYPOTENSION; IC 50; IN VITRO STUDY; LOADING DRUG DOSE; NONHUMAN; PHARMACOKINETICS; STRUCTURE ACTIVITY RELATION; THROMBOCYTE AGGREGATION; THROMBOCYTE FUNCTION; THROMBOSIS;

ANIMALS; CACO-2 CELLS; DISEASE MODELS, ANIMAL; DRUG EVALUATION, PRECLINICAL; FIBRINOLYTIC AGENTS; HALF-LIFE; HUMANS; MICROSOMES, LIVER; PARTIAL THROMBOPLASTIN TIME; PHENYLUREA COMPOUNDS; PLATELET AGGREGATION; PURINERGIC P2Y RECEPTOR ANTAGONISTS; PYRIDINES; RABBITS; RATS; RECEPTORS, PURINERGIC P2Y1; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; THROMBOSIS; UREA; WATER;

ORYCTOLAGUS CUNICULUS; RATTUS;

EID: 84877576404     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.03.125     Document Type: Article

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