Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives : Novel agonists for the CB1 receptor

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 chemis...

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Bibliographic Details
Published in:	European journal of medicinal chemistry Vol. 43; no. 3; pp. 513 - 539
Main Authors:	MOLONEY, Gerard P, ANGUS, James A, ROBERTSON, Alan D, STOERMER, Martin J, ROBINSON, Michael, WRIGHT, Christine E, MCRAE, Ken, CHRISTOPOULOS, Arthur
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier 01-03-2008
Subjects:	Analgesics - chemical synthesis Analgesics - chemistry Analgesics - metabolism Analgesics - pharmacology Animals Binding Sites Biological and medical sciences Cannabinoids - metabolism Drug Design Hydrogen Bonding Hydrophobic and Hydrophilic Interactions Indoles - chemical synthesis Indoles - chemistry Indoles - metabolism Indoles - pharmacology Inhibitory Concentration 50 Medical sciences Mice Miscellaneous Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oxadiazoles - chemical synthesis Oxadiazoles - chemistry Oxadiazoles - metabolism Oxadiazoles - pharmacology Pharmacology. Drug treatments Rats Receptor, Cannabinoid, CB1 - agonists Receptor, Cannabinoid, CB1 - chemistry Receptor, Cannabinoid, CB1 - metabolism Substrate Specificity CB1 cannabinoid receptor Agonist Rat Rodentia Cannabinoid CB1 receptors In vitro Modeling Biological activity Aminoalkylindoles Design Vertebrata CB1 agonists Mammalia Pain Synthesis Animal Molecular model Oxadiazole derivatives Indole derivatives Chemical synthesis Pain control
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Summary:	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.
ISSN:	0223-5234 1768-3254
DOI:	10.1016/j.ejmech.2007.04.007