Quality Control of 4,4-Diethoxybutan-1-amineOn May 5, 2021 ,《Phenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer’s Disease》 appeared in ACS Chemical Neuroscience. The author of the article were Gorecki, Lukas; Uliassi, Elisa; Bartolini, Manuela; Janockova, Jana; Hrabinova, Martina; Hepnarova, Vendula; Prchal, Lukas; Muckova, Lubica; Pejchal, Jaroslav; Karasova, Jana Z.; Mezeiova, Eva; Benkova, Marketa; Kobrlova, Tereza; Soukup, Ondrej; Petralla, Sabrina; Monti, Barbara; Korabecny, Jan; Bolognesi, Maria Laura. The article conveys some information:
Since 2002, no clin. candidate against Alzheimer’s disease has reached the market; hence, an effective therapy is urgently needed. We followed the so-called “”multitarget directed ligand”” approach and designed 36 novel tacrine-phenothiazine heterodimers which were in vitro evaluated for their anticholinesterase properties. The assessment of the structure-activity relationships of such derivatives highlighted compound 1dC as a potent and selective acetylcholinesterase inhibitor with IC50 = 8 nM and 1aA as a potent butyrylcholinesterase inhibitor with IC50 = 15 nM. Selected hybrids, namely, 1aC, 1bC, 1cC, 1dC, and 2dC, showed a significant inhibitory activity toward τ(306-336) peptide aggregation with percent inhibition ranging from 50.5 to 62.1%. Likewise, 1dC and 2dC exerted a remarkable ability to inhibit self-induced Aβ1-42 aggregation. Notwithstanding, in vitro studies displayed cytotoxicity toward HepG2 cells and cerebellar granule neurons; no pathophysiol. abnormality was observed when 1dC was administered to mice at 14 mg/kg (i.p.). 1dC was also able to permeate to the CNS as shown by in vitro and in vivo models. The maximum brain concentration was close to the IC50 value for acetylcholinesterase inhibition with a relatively slow elimination half-time. 1dC showed an acceptable safety and good pharmacokinetic properties and a multifunctional biol. profile. The experimental process involved the reaction of 4,4-Diethoxybutan-1-amine(cas: 6346-09-4Quality Control of 4,4-Diethoxybutan-1-amine)
4,4-Diethoxybutan-1-amine(cas: 6346-09-4) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Quality Control of 4,4-Diethoxybutan-1-amine
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