title: Synthesis and evaluation of a series of aryl[e]fused pyrazolo[4,3-c]pyridines with potential anxiolytic activity.
abstract: A series of pyrazolo[4,3-c]pyridines has been synthesized and evaluated as potential anxiolytic agents. Selected compounds from this series show a pharmacological profile of action different from that of diazepam. A number of the compounds possess higher affinity for central benzodiazepine receptors than diazepam, yet show less anticonvulsant activity and are less sedative. The structure-activity relationships of these potential anxiolytic agents are discussed.
authors.affiliation: Beecham Pharmaceuticals, Medicinal Research Centre, Harlow, Essex, England.
authors.forename: I T
authors.initials: IT
authors.lastname: Forbes
authors.forename: C N
authors.initials: CN
authors.lastname: Johnson
authors.forename: G E
authors.initials: GE
authors.lastname: Jones
authors.forename: J
authors.initials: J
authors.lastname: Loudon
authors.forename: J M
authors.initials: JM
authors.lastname: Nicholass
authors.forename: M
authors.initials: M
authors.lastname: Thompson
authors.forename: N
authors.initials: N
authors.lastname: Upton
mesh_terms: D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D008297:Male; D051379:Mice; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000378:metabolism; D011725:Pyridines / Q000138:chemical synthesis* / Q000378:metabolism; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D014151:Anti-Anxiety Agents; D011720:Pyrazoles; D011725:Pyridines; D011963:Receptors, GABA-A