Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists

Autor:	Jean E. Cottney, Paul Ratcliffe, James Baker, Ruth Fields, John K. Clark, Helen Feilden, Darren Edwards, Grant Wishart, Fiona Jeremiah, Maureen Deehan, Angus John Morrison, Stuart Francis, Louise Evans, Alan Prosser, Robert A. Campbell, Ola Epemolu, Jurgen Schulz, Keneth Davies, Takao Kiyoi, Duncan McArthur, Julia M. Adam, Anna-Marie Easson
Rok vydání:	2010
Předmět:	Agonist Cannabinoid receptor medicine.drug_class medicine.medical_treatment Clinical Biochemistry Pharmaceutical Science Oxadiazole Administration Oral Biological Availability Pharmacology Biochemistry chemistry.chemical_compound Thiadiazoles Receptor Cannabinoid CB1 Heterocyclic Compounds Drug Discovery medicine Animals Molecular Biology Indole test Organic Chemistry Cannabinoid Receptor Agonists Biological activity Rats chemistry Molecular Medicine lipids (amino acids peptides and proteins) Cannabinoid
Zdroj:	Bioorganicmedicinal chemistry letters. 21(6)
ISSN:	1464-3405
Popis:	Novel 3-(1H-indol-3-yl)-1,2,4-oxadiazoles and -thiadiazoles were synthesized and found to be potent CB1 cannabinoid receptor agonists. The oral bioavailability of these compounds could be dramatically improved by optimization studies of the side chains attached to the indole and oxadiazole cores, leading to identification of a CB1 receptor agonist with good oral activity in a range of preclinical models of antinociception and antihyperalgesia.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4a798f1ce53f1985c5d6f38960f220f https://pubmed.ncbi.nlm.nih.gov/21316962 Zobrazit plný text záznamu Full Text from ScienceDirect