1346556-41-9

Upstream product

• 100-58-3 phenylmagnesium bromide 
• 1346556-23-7 1-[(nitrooxy)methyl]cyclopropanecarboxylic acid (4-methyl-5-thiazolyl)phenylmethyl ester 
• 82294-70-0 4-methyl-1,3-thiazole-5-carbaldehyde 
• 1346556-39-5 3-bromo-5-(methoxymethoxy)pyridine 
• 74115-13-2 5-bromopyridine-3-ol 
• 1346556-40-8 3-(methoxymethoxy)-5-[2-(trimethylsilyl)ethynyl]pyridine 
• 103985-97-3 1-(4-methyl-5-thiazolyl)-1-phenylmethanol 

Downstream Products

• 1346556-13-5 5-[1-[(4-methyl-5-thiazolyl)phenylmethyl]-1H-1,2,3-triazol-4-yl]-3-pyridinol 
• 1346556-26-0 C₂₃H₂₀N₆O₅S 
• 1346556-27-1 4-[[5-[1-[(4-methyl-5-thiazolyl)phenylmethyl]-1H-1,2,3-triazol-4-yl]-3-pyridinyl]oxybutane]-1-nitrate 

Relevant academic research and scientific papers

COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE

The present application relates to methods for treatment comprising administering an effect amount of a therapeutic organic compound to a subject need thereof.

Design and synthesis of neuroprotective methylthiazoles and modification as NO-chimeras for neurodegenerative therapy

Learning and memory deficits in Alzheimers disease (AD) result from synaptic failure and neuronal loss, the latter caused in part by excitotoxicity and oxidative stress. A therapeutic approach is described that uses NO-chimeras directed at restoration of both synaptic function and neuroprotection. 4-Methylthiazole (MZ) derivatives were synthesized, based upon a lead neuroprotective pharmacophore acting in part by GABAA receptor potentiation. MZ derivatives were assayed for protection of primary neurons against oxygen-glucose deprivation and excitotoxicity. Selected neuroprotective derivatives were incorporated into NO-chimera prodrugs, coined nomethiazoles. To provide proof of concept for the nomethiazole drug class, selected examples were assayed for restoration of synaptic function in hippocampal slices from AD-transgenic mice, reversal of cognitive deficits, and brain bioavailability of the prodrug and its neuroprotective MZ metabolite. Taken together, the assay data suggest that these chimeric nomethiazoles may be of use in treatment of multiple components of neurodegenerative disorders, such as AD.

COMPOUNDS AND METHODS OF TREATING BRAIN DISORDERS

Nitrated and non-nitrated compounds capable of protecting brain tissue from injury and useful as therapeutic agents to treat neurodegenerative diseases and conditions are disclosed. Methods of using the compounds in therapeutic treatments, and methods of preparing the compounds, also are disclosed.