Design, synthesis, and structure–activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists

Autor:	Morag Ferguson, Jean E. Cottney, Darren Edwards, James Baker, Jim Cairns, Paul Westwood, Fiona Jeremiah, Jason Tierney, Andrea K. Houghton, Mark York, Richard Goodwin, Phillip M. Cowley, Glenn Walker, Ashvin Mistry, Morag Easson, Iain Cumming, Richard Morphy, Wilson Caulfield, Julia M. Adam, Takao Kiyoi, Elizabeth Margaret Moir
Rok vydání:	2010
Předmět:	Pharmacology Indole test Agonist Cannabinoid receptor medicine.drug_class Chemistry medicine.medical_treatment Organic Chemistry Analgesic Pharmaceutical Science Biochemistry Water soluble Design synthesis Drug Discovery medicine Molecular Medicine Potency Cannabinoid
Zdroj:	MedChemComm. 1:54
ISSN:	2040-2511 2040-2503
Popis:	A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded a single confirmed hit with poor water solubility. Structural variations were explored with the aim of introducing water solubility and improving potency. This led to the discovery of Org 28611, a potent, water soluble CB1 receptor agonist, which was selected for clinical evaluation as a potential intravenous analgesic agent.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::50a9771d81118999bd825e636e929401 https://doi.org/10.1039/c0md00022a Zobrazit plný text záznamu