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

doi:10.1016/j.bmcl.2009.04.104

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 rivista › Articolo in rivista › peer 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 originale	Inglese
pagine (da-a)	3199-3203
Numero di pagine	5
Rivista	Bioorganic and Medicinal Chemistry Letters
Volume	19
Numero di pubblicazione	12
DOI	https://doi.org/10.1016/j.bmcl.2009.04.104
Stato di pubblicazione	Pubblicato - 15 giu 2009
Pubblicato esternamente	Sì

Accesso al documento

10.1016/j.bmcl.2009.04.104

Altri file e collegamenti

Link to publication in Scopus

Cita questo

Sasikumar, T. K., Qiang, L., Burnett, D. A., Greenlee, W. J., Li, C., Heimark, L., Pramanik, B., Grilli, M., Bertorelli, R., Lozza, G., & Reggiani, A. (2009). Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain. Bioorganic and Medicinal Chemistry Letters, 19(12), 3199-3203. https://doi.org/10.1016/j.bmcl.2009.04.104

@article{bdbab99d93f54c7d88ec4b8d647d660e,

title = "Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain",

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.",

keywords = "Neuropathic pain, Thienopyrimidine-pyrimidone, Triazafluorenone, Tricyclic thienopyridine-pyrimidone, mGluR1 antagonist",

author = "Sasikumar, \{T. K.\} and Li Qiang and Burnett, \{Duane A.\} and Greenlee, \{William J.\} and Cheng Li and Larry Heimark and Birendra Pramanik and Mariagrazia Grilli and Rosalia Bertorelli and Gianluca Lozza and Angelo Reggiani",

year = "2009",

month = jun,

day = "15",

doi = "10.1016/j.bmcl.2009.04.104",

language = "English",

volume = "19",

pages = "3199--3203",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "12",

}

Sasikumar, TK, Qiang, L, Burnett, DA, Greenlee, WJ, Li, C, Heimark, L, Pramanik, B, Grilli, M, Bertorelli, R, Lozza, G & Reggiani, A 2009, 'Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain', Bioorganic and Medicinal Chemistry Letters, vol. 19, n. 12, pagg. 3199-3203. https://doi.org/10.1016/j.bmcl.2009.04.104

TY - JOUR

T1 - Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain

AU - Sasikumar, T. K.

AU - Qiang, Li

AU - Burnett, Duane A.

AU - Greenlee, William J.

AU - Li, Cheng

AU - Heimark, Larry

AU - Pramanik, Birendra

AU - Grilli, Mariagrazia

AU - Bertorelli, Rosalia

AU - Lozza, Gianluca

AU - Reggiani, Angelo

PY - 2009/6/15

Y1 - 2009/6/15

N2 - 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.

AB - 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.

KW - Neuropathic pain

KW - Thienopyrimidine-pyrimidone

KW - Triazafluorenone

KW - Tricyclic thienopyridine-pyrimidone

KW - mGluR1 antagonist

UR - https://www.scopus.com/pages/publications/65749101021

U2 - 10.1016/j.bmcl.2009.04.104

DO - 10.1016/j.bmcl.2009.04.104

M3 - Article

SN - 0960-894X

VL - 19

SP - 3199

EP - 3203

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 12

ER -

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

Abstract

Accesso al documento

Altri file e collegamenti

Fingerprint

Cita questo