Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 2, Pages 414-418Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.10.028
Keywords
Alzheimer's disease; pyridazine; process chemistry; proinflammatory cytokine; neurodegeneration
Categories
Funding
- Intramural NIH HHS [Z01 AG000260] Funding Source: Medline
- NIA NIH HHS [T32 AG000260, U01 AG028561, AG028561] Funding Source: Medline
- NINDS NIH HHS [NS047586, R01 NS047586] Funding Source: Medline
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We report the development of a novel, aqueous-soluble, safe, small molecule, experimental therapeutic that suppresses injury-induced, proinflammatory cytokine increases in the brain, with resultant attenuation of synaptic protein biomarker loss and improvement in hippocampus-dependent behavioral deficits. A GMP production scheme for the active pharmaceutical ingredient, compound 17, is presented. The development and large-scale availability of this novel compound allow exploration of new, potentially disease-modifying, therapeutic approaches to CNS disorders. (c) 2006 Elsevier Ltd. All rights reserved.
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