The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: Antagonists versus agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 12, 2005, Pages 3020-3023

  Ting, Pauline C ^a   Umland, Shelby P ^a   Aslanian, Robert ^a   Cao, Jianhua ^a   Garlisi, Charles G ^a   Huang, Ying ^a   Jakway, James ^a   Liu, Zhidan ^a   Shah, Himanshu ^a   Tian, Fang ^a   Wan, Yuntao ^a   Shih, Neng Yang ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CHEMOKINE RECEPTOR AGONIST; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR3; PIPERIDINE DERIVATIVE;

AGONIST; ARTICLE; DRUG IDENTIFICATION; DRUG STRUCTURE; DRUG SYNTHESIS; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION;

AMIDES; CHEMOKINES, CC; CHEMOTACTIC FACTORS, EOSINOPHIL; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; PIPERIDINES; PROTEIN BINDING; RECEPTORS, CHEMOKINE; RECEPTORS, HIV; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 19944405095     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.04.054     Document Type: Article

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19. Eotaxin-mediated chemotaxis assay protocol: This assay used BAF3 cells which expressed recombinant human CCR3. The Neuroprobe ChemoTx microplate system with a 5 μm pore size filter was used according to the manufacturer's specifications. Cell chemotaxis in response to 1 nM human eotaxin in the presence and absence of the compound was measured after 3 h incubation at 37°C. Cells which had migrated in response to eotaxin were quantitated using the LDH assay (Promega)