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Volumn 50, Issue 4, 2007, Pages 794-806

Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4- tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524)

(35)  Sturino, Claudio F a   O'Neill, Gary a   Lachance, Nicolas a   Boyd, Michael a   Berthelette, Carl a   Labelle, Marc a   Li, Lianhai a   Roy, Bruno a   Scheigetz, John a   Tsou, Nancy b   Aubin, Yves a   Bateman, Kevin P a   Chauret, Nathalie a   Day, Stephen H a   Lévesque, Jean François a   Seto, Carmai a   Silva, Jose H a   Trimble, Laird A a   Carriere, Marie Claude a   Denis, Danielle a   more..


Author keywords

[No Author keywords available]

Indexed keywords

[4 (4 CHLOROBENZYL) 5 (1 HYDROXYETHYL) 7 (METHYLSULFONYL) 1,2,3,4 TETRAHYDROCYCLOPENTA[B]INDOL 3 YL]ACETIC ACID; [4 (4 CHLOROBENZYL) 7 FLUORO 5 (METHYLSULFONYL) 1,2,3,4 TETRAHYDROCYCLOPENTA[B]INDOL 3 YL]ACETIC ACID; [5 ACETYL 4 (4 CHLOROBENZYL) 7 (METHYLSULFONYL) 1,2,3,4 TETRAHYDROCYCLOPENTA[B]INDOL 3 YL]ACETIC ACID; INDOLEACETIC ACID; MESYLIC ACID DERIVATIVE; MK 0524; PROSTAGLANDIN D2; PROSTAGLANDIN RECEPTOR; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

EID: 33847345910     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0603668     Document Type: Article
Times cited : (172)

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    • 14C radiolabeled 11 and 12 will be reported elsewhere.
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    • The structure of 20, the enantiomer of 13, is as follows: (Diagram presented).
    • The structure of 20, the enantiomer of 13, is as follows: (Diagram presented).
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    • No significant inhibition of the major cyctochrome P450 enzymes (1A2, 3A4, 2D6, 2C9) was observed with 13.
    • No significant inhibition of the major cyctochrome P450 enzymes (1A2, 3A4, 2D6, 2C9) was observed with 13.


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