title: Synthesis and in vivo evaluation of 3,4-disubstituted gababutins.
abstract: 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.
authors.affiliation: Sandwich Laboratories, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. david.blakemore@pfizer.com
authors.forename: David C
authors.initials: DC
authors.lastname: Blakemore
authors.forename: Justin S
authors.initials: JS
authors.lastname: Bryans
authors.forename: Pauline
authors.initials: P
authors.lastname: Carnell
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Field
authors.forename: Natasha
authors.initials: N
authors.lastname: Kinsella
authors.forename: Jack K
authors.initials: JK
authors.lastname: Kinsora
authors.forename: Leonard T
authors.initials: LT
authors.lastname: Meltzer
authors.forename: Simon A
authors.initials: SA
authors.lastname: Osborne
authors.forename: Lisa R
authors.initials: LR
authors.lastname: Thompson
authors.forename: Sophie C
authors.initials: SC
authors.lastname: Williams
mesh_terms: 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
chemical_list: D000588:Amines; D000596:Amino Acids; D014151:Anti-Anxiety Agents; D003509:Cyclohexanecarboxylic Acids; D003517:Cyclopentanes; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin