title: Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor.
abstract: An exploratory chemical effort has been undertaken to develop a novel series of compounds as selective CB(1) agonists. It is hoped that compounds of this type will have clinical utility in pain control, and cerebral ischaemia following stroke or traumatic head injury. We report here medicinal chemistry studies directed towards the investigation of a series of 1-substituted-indole-3-oxadiazoles as potential CB(1) agonists.
authors.affiliation: Department of Medicinal Chemistry, Victorian College of Pharmacy (Monash University), 381 Royal Parade Parkville, Victoria, 3052, Australia. gerard.moloney@vcp.monash.edu.au
authors.forename: Gerard P
authors.initials: GP
authors.lastname: Moloney
authors.forename: James A
authors.initials: JA
authors.lastname: Angus
authors.forename: Alan D
authors.initials: AD
authors.lastname: Robertson
authors.forename: Martin J
authors.initials: MJ
authors.lastname: Stoermer
authors.forename: Michael
authors.initials: M
authors.lastname: Robinson
authors.forename: Christine E
authors.initials: CE
authors.lastname: Wright
authors.forename: Ken
authors.initials: K
authors.lastname: McRae
authors.forename: Arthur
authors.initials: A
authors.lastname: Christopoulos
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001665:Binding Sites; D002186:Cannabinoids / Q000378:metabolism*; D015195:Drug Design; D006860:Hydrogen Bonding; D057927:Hydrophobic and Hydrophilic Interactions; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D051379:Mice; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists* / Q000737:chemistry / Q000378:metabolism; D013379:Substrate Specificity
chemical_list: D000700:Analgesics; D002186:Cannabinoids; D007211:Indoles; D010069:Oxadiazoles; D043884:Receptor, Cannabinoid, CB1