Comparison between two classes of selective EP(3) antagonists and their biological activities

Autor: Kathleen M. Metters, Deborah Slipetz, Nicolas Lachance, Marc Labelle, Danielle Denis, Chi-Chung Chan, Michel Gallant, Robert Zamboni, Sonia Lamontagne, Gillian Greig, Yves Gareau, Nicole Sawyer, Nathalie Tremblay, Helene Juteau, Karine Houde, Chun Li, Marie-Claude Carrière, Nathalie Chauret, Robert Gordon, Michel Belley
Rok vydání: 2006
Předmět:
Zdroj: Bioorganicmedicinal chemistry letters. 16(21)
ISSN: 0960-894X
Popis: Two different series of very potent and selective EP(3) antagonists have been reported: a novel series of ortho-substituted cinnamic acids [Belley, M., Gallant, M., Roy, B., Houde, K., Lachance, N., Labelle, M., Trimble, L., Chauret, N., Li, C., Sawyer, N., Tremblay, N., Lamontagne, S., Carriere, M.-C., Denis, D., Greig, G. M., Slipetz, D., Metters, K. M., Gordon, R., Chan, C. C., Zamboni, R. J. Bioorg. Med. Chem. Lett.2005, 15, 527] and the acylsulfonamides of ortho-(arylmethyl)cinnamates. [(a) Juteau, H., Gareau, Y., Labelle, M., Sturino, C. F., Sawyer, N., Tremblay, N., Lamontagne, S., Carriere, M.-C., Denis, D., Metters, K. M. Bioorg. Med. Chem. 2001, 9, 1977; (b) Juteau, H., Gareau, Y., Labelle, M., Lamontagne, S., Tremblay, N., Carriere, M.-C., Denis, D., Sawyer, N., Metters, K. M. Bioorg. Med. Chem. Lett.2001, 11, 747] The structural differences between the two series, along with their biological activity in vivo, in vitro, and metabolism, are analyzed. Some of those compounds, including hybrids containing the best structural features of both series, possess K(i) as low as 0.6 nM on the EP(3) receptor.
Databáze: OpenAIRE
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