title: Synthesis and in vivo evaluation of 3-substituted gababutins.
abstract: 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.
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: Nicola E A
authors.initials: NE
authors.lastname: Chessum
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: Simon A
authors.initials: SA
authors.lastname: Osborne
authors.forename: Sophie C
authors.initials: SC
authors.lastname: Williams
mesh_terms: 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
chemical_list: 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