From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: The discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 2, 2008, Pages 576-585

  Santella III, Joseph B ^a   Gardner, Daniel S ^a   Yao, Wenqing ^a   Shi, Chongsheng ^a   Reddy, Prabhakar ^a   Tebben, Andrew J ^a   DeLucca, George V ^a   Wacker, Dean A ^a   Watson, Paul S ^a   Welch, Patricia K ^a   Wadman, Eric A ^a   Davies, Paul ^a   Solomon, Kimberly A ^a   Graden, Dani M ^a   Yeleswaram, Swamy ^a   Mandlekar, Sandhya ^a   Kariv, Ilona ^a   Decicco, Carl P ^a   Ko, Soo S ^a   Carter, Percy H ^a   Duncia, John V ^a   more..

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Ab initio; Acyclic scaffold; Asthma; BMS 639623; CCR3 antagonist; Conformational analysis; Development candidate; Eosinophil chemotaxis

Indexed keywords

ALPHA METHYL BETA HYDROXYPROPYLUREA; BMS 639623; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR3; CYCLOHEXANE; CYTOCHROME P450 2D6; METHYL GROUP; UNCLASSIFIED DRUG;

AB INITIO CALCULATION; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; CHEMOTAXIS; COMPUTER MODEL; CONFORMATIONAL TRANSITION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; EOSINOPHIL; IC 50; MOUSE; NONHUMAN; RAT;

ADMINISTRATION, ORAL; ANIMALS; CHEMOTAXIS, LEUKOCYTE; CYTOCHROME P-450 ENZYME SYSTEM; DOGS; EOSINOPHILS; HYDROGEN BONDING; MICE; MOLECULAR CONFORMATION; PIPERIDINES; RATS; RECEPTORS, CCR3; STRUCTURE-ACTIVITY RELATIONSHIP; UREA;

EID: 38349002583     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.11.067     Document Type: Article

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