18 research outputs found
Aziridine Ring Opening for the Synthesis of Sphingolipid Analogues: Inhibitors of Sphingolipid-Metabolizing Enzymes
Full text linkIdentification and Electrophysiological Evaluation of 2-Methylbenzamide Derivatives as Na v
No full textIdentification and Electrophysiological Evaluation of 2‑Methylbenzamide Derivatives as Na<sub>v</sub>1.1 Modulators
No full textVoltage-gated sodium channels (Na<sub>v</sub>) are crucial to the
initiation and propagation of action potentials (APs) in electrically
excitable cells, and during the past decades they have received considerable
attention due to their therapeutic potential. Here, we report for
the first time the synthesis and the electrophysiological evaluation
of 16 ligands based on a 2-methylbenzamide scaffold that have been
identified as Na<sub>v</sub>1.1 modulators. Among these compounds, <i>N</i>,<i>N</i>′-(1,3-phenylene)ÂbisÂ(2-methylbenzamide)
(<b>3a</b>) has been selected and evaluated in ex-vivo experiments
in order to estimate the activation impact of such a compound profile.
It appears that <b>3a</b> increases the Na<sub>v</sub>1.1 channel
activity although its overall impact remains moderate. Altogether,
our preliminary results provide new insights into the development
of small molecule activators targeting specifically Na<sub>v</sub>1.1 channels to design potential drugs for treating CNS diseases
Aqabamycins A–G: novel nitro maleimides from a marine Vibrio species: II. Structure elucidation*
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Expedite Protocol for Construction of Chiral Regioselectively N-Protected Monosubstituted Piperazine, 1,4-Diazepane, and 1,4-Diazocane Building Blocks
No full textRegio- and Chemoselective Zincation of Sensitive and Moderately Activated Aromatics and Heteroaromatics Using TMPZnCl·LiCl
No full textChemo- and Regioselective Functionalization of Nortrilobolide: Application for Semisynthesis of the Natural Product 2-Acetoxytrilobolide
No full textSynthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists
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