title: Synthesis and in vivo evaluation of bicyclic gababutins.
abstract: Synthesis of a number of bicyclic five-membered ring derivatives of gabapentin led to the identification of two compounds, (-)-(11A) and (20A) which both had an excellent level of potency against alpha(2)delta and were profiled in an in vivo model of neuropathic pain.
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: Christopher L
authors.initials: CL
authors.lastname: Carr
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: Simon A
authors.initials: SA
authors.lastname: Osborne
authors.forename: Andrew N
authors.initials: AN
authors.lastname: Warren
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 / Q000493:pharmacokinetics; D000818:Animals; D001812:Blood-Brain Barrier / Q000378:metabolism; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D003509:Cyclohexanecarboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D000077206:Gabapentin; D009437:Neuralgia / Q000188:drug therapy; D010147:Pain Measurement; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D005680:gamma-Aminobutyric Acid / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D000588:Amines; D000596:Amino Acids; D001643:Bridged Bicyclo Compounds; D003509:Cyclohexanecarboxylic Acids; D005680:gamma-Aminobutyric Acid; D000077206:Gabapentin