Publications by authors named "Caroline Beaufour"
The synthesis and biological evaluation on AMPA and kainate receptors of new examples of 3,4-dihydro-2H-1,2,4-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxides is described. The introduction of a cyclopropyl chain instead of an ethyl chain at the 4-position of the thiadiazine ring was found to dramatically improve the potentiator activity on AMPA receptors, with compound 32 (BPAM395) expressing in vitro activity on AMPARs (EC2x = 0.24 μM) close to that of the reference 4-cyclopropyl-substituted benzothiadiazine dioxide 10 (BPAM344).
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- Positive allosteric modulators of AMPA receptors are being researched as potential new treatments for neurodegenerative diseases like Alzheimer's, Parkinson's, ADHD, depression, and schizophrenia.
- This study examines new compounds based on 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides with variations in alkyl substituents to enhance effectiveness.
- The compound 7-chloro-4-cyclopropyl-2-fluoromethyl-3,4-dihydro-4H-1,2,4-benzothiadiazine 1,1-dioxide (15e) shows high potency, a good safety profile