2-Mercaptoimidazoles, a new class of potent CCR2 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 3, 2005, Pages 497-500

  Van Lommen, Guy ^a   Doyon, Julien ^a   Coesemans, Erwin ^a   Boeckx, Staf ^a   Cools, Marina ^b   Buntinx, Mieke ^a   Hermans, Bart ^a   VanWauwe, Jean ^a  

^a Johnson Johnson Pharmaceutical R D   (Belgium)

^b Barrier Therapeutics NV   (Belgium)

Author keywords

CCR2 antagonists; Mercaptoimidazoles

Indexed keywords

CHEMOKINE RECEPTOR ANTAGONIST; IMIDAZOLE DERIVATIVE;

ARTICLE; CALCIUM TRANSPORT; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IC 50; STRUCTURE ACTIVITY RELATION;

CALCIUM SIGNALING; CELL LINE; CHEMOKINE CCL2; ETHYLENETHIOUREA; HUMANS; IMIDAZOLES; INHIBITORY CONCENTRATION 50; RECEPTORS, CHEMOKINE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 12444298917     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.11.064     Document Type: Article

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15. 2+ concentration were measured using the Fluorescent Imaging Plate Reader (FLIPR, Molecular Devices, Munich, Germany). Fluorescence was recorded every second from 10 s before the addition of the MCP-1 untill 2 min after the addition (first minute: 60 records with 1 s intervals, second minute: 20 records with 3 s intervals). The maximal fluorescence obtained during this time frame was used for further calculations
16. 2. After 2 h incubation, the nonmigrated cells were removed from the top of the filter by gently wiping the filter with a tissue. The migrated cells were measured using a fluorescent plate reader (excitation, 485 nm; emission, 538 nm). The chemotactic response is expressed as chemotactic index (CI), being the ratio of the means of migrated cells in the presence of MCP-1 and the means of migrated cells in the absence of chemokine