Synthesis and in vivo evaluation of 3,4-disubstituted gababutins.
A range of 3,4-alkylated five-membered ring derivatives of gabapentin were synthesised. One compound (21) had an excellent level of potency against alpha(2)delta and was 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
Field
Mark J
MJ
Kinsella
Natasha
N
Kinsora
Jack K
JK
Meltzer
Leonard T
LT
Osborne
Simon A
SA
Thompson
Lisa R
LR
Williams
Sophie C
SC
D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000596:Amino Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D003509:Cyclohexanecarboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004195:Disease Models, Animal; D000077206:Gabapentin; D006930:Hyperalgesia / Q000139:chemically induced / Q000188:drug therapy; D051381:Rats; D005680:gamma-Aminobutyric Acid / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
D000588:Amines; D000596:Amino Acids; D014151:Anti-Anxiety Agents; D003509:Cyclohexanecarboxylic Acids; D003517:Cyclopentanes; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin