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 superior potency against the α2δ calcium subunit. Diastereoisomeric compounds, ( 16) and ( 22), were profiled in in vivo models of pain and anxiety and proved to have different levels...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010, Vol.20 (1), p.362-365
Hauptverfasser:	Blakemore, David C., Bryans, Justin S., Carnell, Pauline, Chessum, Nicola E.A., Field, Mark J., Kinsella, Natasha, Kinsora, Jack K., Osborne, Simon A., Williams, Sophie C.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amines - chemical synthesis Amines - chemistry Amines - pharmacology Amino Acids - chemical synthesis Amino Acids - chemistry Amino Acids - pharmacology Analgesics Animals Anti-Anxiety Agents - chemical synthesis Anti-Anxiety Agents - chemistry Anti-Anxiety Agents - pharmacology Anxiety Biological and medical sciences Calcium Channels - metabolism Carrageenan - pharmacology Cyclohexanecarboxylic Acids - chemical synthesis Cyclohexanecarboxylic Acids - chemistry Cyclohexanecarboxylic Acids - pharmacology Cyclopentanes - chemical synthesis Cyclopentanes - chemistry Cyclopentanes - pharmacology Gababutin Gabapentin gamma-Aminobutyric Acid - chemical synthesis gamma-Aminobutyric Acid - chemistry gamma-Aminobutyric Acid - pharmacology Hyperalgesia - chemically induced Hyperalgesia - drug therapy Medical sciences Neuropharmacology Pain Pharmacology. Drug treatments Pregabalin Psycholeptics: tranquillizer, neuroleptic Psychology. Psychoanalysis. Psychiatry Psychopharmacology Rats Stereoisomerism
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	A range of 3-alkylated five-membered ring derivatives of Gabapentin were synthesized and several were found to have superior potency against the α2δ calcium subunit. Diastereoisomeric compounds, ( 16) and ( 22), were profiled in in vivo models of pain and anxiety and proved to have different levels of efficacy in the two models. 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 α2δ calcium subunit of a voltage-gated calcium channel. Two compounds were profiled in in vivo models of pain and anxiety.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.10.089