Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound

Salida Mirzoeva; Anu Sawkar; Magdalena Zasadzki; Ling Guo; Anastasia V. Velentza; Vincent Dunlap; Jean Jacques Bourguignonl; Helena Ramstrom; Jacques Haiech; Linda J. Van Eldik; D. M. Watterson

doi:10.1021/jm015573g

Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound

Salida Mirzoeva, Anu Sawkar, Magdalena Zasadzki, Ling Guo, Anastasia V. Velentza, Vincent Dunlap, Jean Jacques Bourguignonl, Helena Ramstrom, Jacques Haiech, Linda J. Van Eldik, D. M. Watterson^*

^*Corresponding author for this work

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

60 Scopus citations

Abstract

Excessive glial activation, with overproduction of cytokines and oxidative stress products, is detrimental and a hallmark of neurodegenerative disease pathology. Suppression of glial activation is a potential therapeutic approach, and protein kinases are targets of some antiinflammatory drugs. To address an unmet need for selective inhibitors of glial activation, we developed a novel 3-amino-6-phenylpyridazine derivative that selectively blocks increased IL-1β, iNOS, and NO production by activated glia, without inhibition of potentially beneficial glial functions.

Original language	English (US)
Pages (from-to)	563-566
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	45
Issue number	3
DOIs	https://doi.org/10.1021/jm015573g
State	Published - Jan 31 2002

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ASJC Scopus subject areas

Drug Discovery
Molecular Medicine

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abstract = "Excessive glial activation, with overproduction of cytokines and oxidative stress products, is detrimental and a hallmark of neurodegenerative disease pathology. Suppression of glial activation is a potential therapeutic approach, and protein kinases are targets of some antiinflammatory drugs. To address an unmet need for selective inhibitors of glial activation, we developed a novel 3-amino-6-phenylpyridazine derivative that selectively blocks increased IL-1β, iNOS, and NO production by activated glia, without inhibition of potentially beneficial glial functions.",

author = "Salida Mirzoeva and Anu Sawkar and Magdalena Zasadzki and Ling Guo and Velentza, {Anastasia V.} and Vincent Dunlap and Bourguignonl, {Jean Jacques} and Helena Ramstrom and Jacques Haiech and {Van Eldik}, {Linda J.} and Watterson, {D. M.}",

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T1 - Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound

AU - Mirzoeva, Salida

AU - Sawkar, Anu

AU - Zasadzki, Magdalena

AU - Guo, Ling

AU - Velentza, Anastasia V.

AU - Dunlap, Vincent

AU - Bourguignonl, Jean Jacques

AU - Ramstrom, Helena

AU - Haiech, Jacques

AU - Van Eldik, Linda J.

AU - Watterson, D. M.

PY - 2002/1/31

Y1 - 2002/1/31

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AB - Excessive glial activation, with overproduction of cytokines and oxidative stress products, is detrimental and a hallmark of neurodegenerative disease pathology. Suppression of glial activation is a potential therapeutic approach, and protein kinases are targets of some antiinflammatory drugs. To address an unmet need for selective inhibitors of glial activation, we developed a novel 3-amino-6-phenylpyridazine derivative that selectively blocks increased IL-1β, iNOS, and NO production by activated glia, without inhibition of potentially beneficial glial functions.

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Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound

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