Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain

T. K. Sasikumar, Li Qiang, Duane A. Burnett, William J. Greenlee, Cheng Li, Larry Heimark, Birendra Pramanik, Mariagrazia Grilli, Rosalia Bertorelli, Gianluca Lozza, Angelo Reggiani

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

Abstract

Introduction of small unsaturated alkylamino groups at the 4-position of the A-ring of the tricyclic framework (triazafluorenone) afforded extremely potent and selective mGluR1 antagonists with desirable properties. Compounds 11q and 11s are active in the SNL pain model with ED50s 3.3 and 6.4 mg/kg respectively. Metabolic outcome of propargyl amino moiety was studied.

Lingua originaleInglese
pagine (da-a)3199-3203
Numero di pagine5
RivistaBioorganic and Medicinal Chemistry Letters
Volume19
Numero di pubblicazione12
DOI
Stato di pubblicazionePubblicato - 15 giu 2009
Pubblicato esternamente

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