Synthesis and evaluation of a series of aryl[e]fused pyrazolo[4,3-c]pyridines with potential anxiolytic activity.
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.
Forbes
I T
IT
Beecham Pharmaceuticals, Medicinal Research Centre, Harlow, Essex, England.
Johnson
C N
CN
Jones
G E
GE
Loudon
J
J
Nicholass
J M
JM
Thompson
M
M
Upton
N
N
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
D014151:Anti-Anxiety Agents; D011720:Pyrazoles; D011725:Pyridines; D011963:Receptors, GABA-A