Optimization of sphingosine-1-phosphate-1 receptor agonists: Effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles

Journal of Medicinal Chemistry

Volumn 57, Issue 24, 2014, Pages 10424-10442

  Skidmore, John ^a   Heer, Jag ^a   Johnson, Christopher N ^a   Norton, David ^a   Redshaw, Sally ^a   Sweeting, Jennifer ^a   Hurst, David ^a   Cridland, Andrew ^a   Vesey, David ^a   Wall, Ian ^a   Ahmed, Mahmood ^b   Rivers, Dean ^b   Myatt, James ^a   Giblin, Gerard ^a   Philpott, Karen ^a   Kumar, Umesh ^a   Stevens, Alexander ^a   Bit, Rino A ^a   Haynes, Andrea ^a   Taylor, Simon ^a   Watson, Robert ^a   Witherington, Jason ^a   Demont, Emmanuel ^a   Heightman, Tom D ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b Immuno Inflammation Center of Excellence for Drug Discovery GlaxoSmithKline ^*  (Singapore)

Author keywords

[No Author keywords available]

Indexed keywords

AMPHOLYTE; IMMUNOMODULATING AGENT; SIPONIMOD; CARBOXYLIC ACID; HETEROCYCLIC COMPOUND; IMMUNOSUPPRESSIVE AGENT; SPHINGOSINE 1 PHOSPHATE RECEPTOR;

AGONIST; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG CONFORMATION; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG SOLUBILITY; DRUG TISSUE LEVEL; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; IN VIVO STUDY; INTRINSIC CLEARANCE; LIPOPHILICITY; LYMPHOCYTOPENIA; MACACA FASCICULARIS; MALE; MOUSE; NONHUMAN; PERIPHERAL LYMPHOCYTE; PHARMACOPHORE; PHYSICAL CHEMISTRY; PLASMA PROTEIN BINDING; RAT; STEREOSPECIFICITY; VOLUME OF DISTRIBUTION; AGONISTS; ANIMAL; CELL CULTURE; CHEMICAL STRUCTURE; CHEMISTRY; CYTOLOGY; DRUG EFFECTS; LEWIS RAT; LYMPHOCYTE; STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ANIMALS; CARBOXYLIC ACIDS; CELLS, CULTURED; HETEROCYCLIC COMPOUNDS; IMMUNOSUPPRESSIVE AGENTS; LYMPHOCYTES; MALE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; RATS, INBRED LEW; RECEPTORS, LYSOSPHINGOLIPID; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84920164873     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5010336     Document Type: Article

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