《Rational design of small molecules able to inhibit α-synuclein amyloid aggregation for the treatment of Parkinson′s disease》 was written by Vittorio, Serena; Adornato, Ilenia; Gitto, Rosaria; Pena-Diaz, Samuel; Ventura, Salvador; De Luca, Laura. Category: chlorides-buliding-blocks And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020. The article conveys some information:
Parkinson′s disease is one of the most common neurodegenerative disorders in elderly age. One of the mechanisms involved in the neurodegeneration appears related to the aggregation of the presynaptic protein alpha synuclein (α-syn) into toxic oligomers and fibrils. To date, no highly effective treatment is currently available; therefore, there is an increasing interest in the search of new therapeutic tools. The modulation of α-syn aggregation represents an emergent and promising disease-modifying strategy for reducing or blocking the neurodegenerative process. Herein, by combining in silico and in vitro screenings we initially identified 3-(cinnamylsulfanyl)-5-(4-pyridinyl)-1,2,4-triazol-4-amine () as α-syn aggregation inhibitor that was then considered a promising hit for the further design of a new series of small mols. Therefore, we rationally designed new hit-derivatives that were synthesized and evaluated by biol. assays. Lastly, the binding mode of the newer inhibitors was predicted by docking studies. In the experiment, the researchers used 1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7Category: chlorides-buliding-blocks)
1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7) undergoes carbonylation in the presence of dimer of chloro(1,5-cyclooctadiene)rhodium(I) to yield the corresponding phenylacetic acid.Category: chlorides-buliding-blocks It can be synthesized by reacting 4-chlorobenzyl alcohol with bromodimethylsulfonium bromide (BDMS) It can also be synthesized by refluxing a mixture of 4-chlorobenzaldehyde, chlorotrimethylsilane, 1,1,3,3-tetramethyldisiloxane and lithium bromide.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics