Identification of an indole series of prostaglandin D2 receptor antagonists

A novel indole series of PGD2 receptor (DP receptor) antagonists is presented. Optimization of this series led to the identification of potent and selective DP receptor antagonists. In particular, antagonists 35 and 36 were identified with Ki values of 2.6 and 1.8 nM, respectively. These two antagon...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (11), p.3043-3048
Hauptverfasser:	STURINO, Claudio F, LACHANCE, Nicolas, CAUCHON, Elizabeth, CARRIERE, Marie-Claude, DENIS, Danielle, GREIG, Gillian, KARGMAN, Stacia, LAMONTAGNE, Sonia, MATHIEU, Marie-Claude, SAWYER, Nicole, SLIPETZ, Deborah, O'NEILL, Gary, BOYD, Michael, ZHAOYIN WANG, ZAMBONI, Robert, METTERS, Kathleen M, YOUNG, Robert N, BERTHELETTE, Carl, LABELLE, Marc, LIANHAI LI, ROY, Bruno, SCHEIGETZ, John, TSOU, Nancy, BRIDEAU, Christine
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Histamine and antagonists. Allergy Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Medical sciences Molecular Structure Pharmacology. Drug treatments Receptors, Immunologic - antagonists & inhibitors Receptors, Immunologic - metabolism Receptors, Prostaglandin - antagonists & inhibitors Receptors, Prostaglandin - metabolism Safrole - analogs & derivatives Safrole - chemistry Structure-Activity Relationship
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