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Small Molecules in Development for the Treatment of Spinal Muscular Atrophy.
Both repurposed drugs and small-molecule compounds discovered following medicinal chemistry optimization for the potential treatment of SMA are reviewed.
Restored glial glutamate transporter EAAT2 function as a potential therapeutic approach for Alzheimer’s disease
Takahashi et al. demonstrate that restoring glial glutamate transporter EAAT2 function improves cognitive functions and synaptic integrity while reducing amyloid plaques in a sustained fashion after…
Barcoded viral tracing of single-cell interactions in central nervous system inflammation
RABID-seq identified the axon guidance molecules Sema4D-PlexinB2 and EphrinB3-EphB3 as mediators of microglia-astrocyte interactions that promote CNS pathology in experimental autoimmune encephalomyelitis and, potentially, multiple sclerosis.
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
- X. Zhang, K. Hodgetts, A. Thurkauf
- Chemistry, PsychologyJournal of medicinal chemistry
- 30 September 2000
The dopaminergic receptor profile of a series of trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines was examined. Aromatic substitution patterns were varied with the goal of identifying a…
Discovery of a Small Molecule Probe That Post-Translationally Stabilizes the Survival Motor Neuron Protein for the Treatment of Spinal Muscular Atrophy.
This series post-translationally stabilizes the SMN protein, unrelated to global proteasome or autophagy inhibition, revealing a novel therapeutic mechanism that should complement other modalities for treatment of SMA.
The Role of Fluorine in the Discovery and Optimization of CNS Agents: Modulation of Drug-Like Properties
Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
The design and synthesis of a series of novel TRPV1 antagonists with a variety of different 6,6-heterocyclic cores is described, and an extensive evaluation of the pharmacological and pharmacokinetic properties of a number of these compounds is reported.
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.
CLEAVAGE OR ACETYL-DE-ALKYLATION OF 4-METHOXYBENZYL (MPM)ETHERS USING ACETIC ACID
Abstract Aryl (4-methoxyphenyl)methyl (MPM) ethers are cleaved by heating with acetic acid for a few hours at 90°C, producing the corresponding phenols and (4-methoxyphenyl)methyl acetate. Under the…