Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 4, 2006, Pages 1065-1069

  Shue, Ho Jane ^a   Chen, Xiao ^a   Schwerdt, John H ^a   Paliwal, Sunil ^a   Blythin, David J ^a   Lin, Ling ^a   Gu, Danlin ^a   Wang, Cheng ^a   Reichard, Gregory A ^a,b   Wang, Hongwu ^a   Piwinski, John J ^a   Duffy, Ruth A ^a   Lachowicz, Jean E ^a   Coffin, Vicki L ^a   Nomeir, Amin A ^a   Morgan, Cynthia A ^a   Varty, Geoffrey B ^a   Shih, Neng Yang ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b PFIZER INC   (United States)

Author keywords

Improved potency; NK1 antagonist; Sustained in vivo activity

Indexed keywords

NEUROKININ 1 RECEPTOR ANTAGONIST; SCH 388714; UNCLASSIFIED DRUG; UREA DERIVATIVE;

ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; DRUG BIOAVAILABILITY; DRUG CONFORMATION; DRUG INHIBITION; DRUG POTENCY; GERBIL; IN VIVO STUDY; NONHUMAN; RAT; RECEPTOR BINDING; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

ANIMALS; ANTI-ANXIETY AGENTS; BENZYL ALCOHOLS; CRYSTALLOGRAPHY, X-RAY; DRUG EVALUATION, PRECLINICAL; FLUORINE; GERBILLINAE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; MOTOR ACTIVITY; RECEPTORS, NEUROKININ-1; STRUCTURE-ACTIVITY RELATIONSHIP; UREA;

ANIMALIA; GERBILLINAE;

EID: 30344434044     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.10.072     Document Type: Article

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