60553-33-5Relevant academic research and scientific papers
SMALL MOLECULES THAT TARGET THE RNA THAT CAUSES ALS
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Paragraph 00257-00258, (2022/04/03)
Disclosed herein are compounds that selectively bind an expanded transcribed repeat r(G4C2)exp, prevent sequestration of RNA-binding proteins, and inhibit translation of repeat associated non-ATG (RAN) translation responsible for generation of toxic dipeptide repeats underlying diseases such as amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). The compounds and their pharmaceutical compositions are useful in treating a disease or condition characterized by an expanded G4C2 repeat RNA (r(G4C2)exp), such as ALS and FTD.
Synthesis and in vivo and in vitro evaluation of isoarecolone and derivatives
Beach, J. Warren,Damaj, M. Imad,Jonnala, Ramamohana R.,Terry Jr., Alvin V.,Buccafusco, Jerry J.
, p. 510 - 522 (2007/10/03)
The synthesis of the N-ethyl and N-phenylethyl derivatives of isoarecolone are described. These compounds were evaluated in vitro for their ability to displace [3H](±)epibatidine and/or [3H](-) nicotine from nicotinic receptors derived from rat cerebral cortex and their ability to inhibit acetylcholinesterase. The N-ethyl derivative and isoarecolone were evaluated in vivo for their antinociceptive, hypothermia and hypomotility activity in mice. The in vivo activity of isoareeolone was found to the reversible by mecamylamine, however the N-ethyl derivative was found to be insensitive to blockade by mecamylamine.
An Improved Synthesis of 1-(1,2,3,6-Tetrahydro-1-methyl-4- Pyridinyl)ethanone, Isoarecolone
Beach, J. Warren
, p. 1861 - 1863 (2007/10/03)
A convenient synthesis of 1-(1,2,3,6-tetrahydro-1-methyl-4-pyridinyl)ethanone, isoarecolone, starting with 4-acetylpyridine is presented. 4-Acetylpyridine was protected as the ketal followed by reaction with iodomethane to give the quaterary salt. The quaterary salt was reduced with sodium borohydride followed by deprotection to give isoarecolone in 80% overall yield.
