Synthesis and in vivo evaluation of 3-substituted gababutins.
A range of 3-alkylated five-membered ring derivatives of Gabapentin were synthesized and several were found to have good levels of potency against the alpha2delta calcium subunit of a voltage-gated calcium channel. Two compounds were profiled in in vivo models of pain and anxiety.
Blakemore
David C
DC
Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK. david.blakemore@pfizer.com
Bryans
Justin S
JS
Carnell
Pauline
P
Chessum
Nicola E A
NE
Field
Mark J
MJ
Kinsella
Natasha
N
Kinsora
Jack K
JK
Osborne
Simon A
SA
Williams
Sophie C
SC
D000588:Amines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000596:Amino Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015220:Calcium Channels / Q000378:metabolism; D002351:Carrageenan / Q000494:pharmacology; D003509:Cyclohexanecarboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000077206:Gabapentin; D006930:Hyperalgesia / Q000139:chemically induced / Q000188:drug therapy; D051381:Rats; D013237:Stereoisomerism; D005680:gamma-Aminobutyric Acid / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000588:Amines; D000596:Amino Acids; D014151:Anti-Anxiety Agents; D015220:Calcium Channels; D003509:Cyclohexanecarboxylic Acids; D003517:Cyclopentanes; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin; D002351:Carrageenan