Utilization of an intramolecular hydrogen bond to increase the CNS penetration of an NK1 receptor antagonist

Journal of Medicinal Chemistry

Volumn 44, Issue 14, 2001, Pages 2276-2285

  Ashwood, V A ^a   Field, M J ^a   Horwell, D C ^a   Julien Larose, C ^b   Lewthwaite, R A ^a   McCleary, S ^a   Pritchard, M C ^a   Raphy, J ^a   Singh, L ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

[1 (1H INDOL 3 YLMETHYL) 1 METHYL 2 OXO 2 [(1 PHENYLETHYL)AMINO]ETHYL]CARBAMIC ACID BENZO[B]FURAN 2 YLMETHYL ESTER; [1 DIMETHYLAMINOMETHYL 2 (1H INDOL 3 YL) 1 (1 PHENYLETHYLCARBAMOYL)ETHYL]CARBAMIC ACID BENZOFURAN 2YLMETHYL ESTER; [2 (1H INDOL 3 YL) 1 METHYL 1 (1 PHENYLETHYLCARBAMOYL)ETHYL]CARBAMIC ACID BENZOFURAN 2 YLMETHYL ESTER; NEUROKININ; NEUROKININ 1 RECEPTOR; NEUROKININ 1 RECEPTOR ANTAGONIST; NEUROKININ 2 RECEPTOR; NEUROKININ 3 RECEPTOR; PD 174424; RECEPTOR SUBTYPE; TACHYKININ; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BLOOD BRAIN BARRIER; CENTRAL NERVOUS SYSTEM; CRYSTAL STRUCTURE; DIASTEREOISOMER; HYDROGEN BOND; LIPOPHILICITY; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; RECEPTOR BINDING; SYNTHESIS; TEMPERATURE DEPENDENCE; X RAY CRYSTALLOGRAPHY;

ANIMALS; BENZOFURANS; BRAIN; CARBAMATES; CRYSTALLOGRAPHY, X-RAY; GERBILLINAE; HINDLIMB; HUMANS; HYDROGEN BONDING; INDOLES; INJECTIONS, INTRAVENTRICULAR; INJECTIONS, SUBCUTANEOUS; MODELS, MOLECULAR; RECEPTORS, NEUROKININ-1; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTANCE P;

EID: 0035811455     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010825z     Document Type: Article

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