A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties

T. K. Sasikumar; Li Qiang; Duane A. Burnett; William J. Greenlee; Cheng Li; Mariagrazia Grilli; Rosalia Bertorelli; Gianluca Lozza; Angelo Reggiani

doi:10.1016/j.bmcl.2010.03.004

A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties

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

Research output: Contribution to journal › Article › peer-review

Abstract

A-ring modifications on the triazafluorenone core structure were investigated. Five membered heterocycles such as pyrazoles and isothiazoles are not tolerated. It has been found that the pyrimidine nucleus was very well tolerated on the left hand side. Amino pyrimidine compounds 24 and 27 showed acceptable PK profile with significant brain penetration. Compound 9 served as a versatile intermediate for a number of chemical transformations.

Original language	English
Pages (from-to)	2474-2477
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2010.03.004
Publication status	Published - 15 Apr 2010
Externally published	Yes

Keywords

Neuropathic pain
mGluR1 antagonist

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10.1016/j.bmcl.2010.03.004

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title = "A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties",

abstract = "A-ring modifications on the triazafluorenone core structure were investigated. Five membered heterocycles such as pyrazoles and isothiazoles are not tolerated. It has been found that the pyrimidine nucleus was very well tolerated on the left hand side. Amino pyrimidine compounds 24 and 27 showed acceptable PK profile with significant brain penetration. Compound 9 served as a versatile intermediate for a number of chemical transformations.",

keywords = "Neuropathic pain, mGluR1 antagonist",

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

year = "2010",

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doi = "10.1016/j.bmcl.2010.03.004",

language = "English",

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TY - JOUR

T1 - A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties

AU - Sasikumar, T. K.

AU - Qiang, Li

AU - Burnett, Duane A.

AU - Greenlee, William J.

AU - Li, Cheng

AU - Grilli, Mariagrazia

AU - Bertorelli, Rosalia

AU - Lozza, Gianluca

AU - Reggiani, Angelo

PY - 2010/4/15

Y1 - 2010/4/15

N2 - A-ring modifications on the triazafluorenone core structure were investigated. Five membered heterocycles such as pyrazoles and isothiazoles are not tolerated. It has been found that the pyrimidine nucleus was very well tolerated on the left hand side. Amino pyrimidine compounds 24 and 27 showed acceptable PK profile with significant brain penetration. Compound 9 served as a versatile intermediate for a number of chemical transformations.

AB - A-ring modifications on the triazafluorenone core structure were investigated. Five membered heterocycles such as pyrazoles and isothiazoles are not tolerated. It has been found that the pyrimidine nucleus was very well tolerated on the left hand side. Amino pyrimidine compounds 24 and 27 showed acceptable PK profile with significant brain penetration. Compound 9 served as a versatile intermediate for a number of chemical transformations.

KW - Neuropathic pain

KW - mGluR1 antagonist

UR - https://www.scopus.com/pages/publications/77950051353

U2 - 10.1016/j.bmcl.2010.03.004

DO - 10.1016/j.bmcl.2010.03.004

M3 - Article

SN - 0960-894X

VL - 20

SP - 2474

EP - 2477

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

A-ring modifications on the triazafluorenone core structure and their mGluR1 antagonist properties

Abstract

Keywords

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