Structure-activity relationship around PI-2620 highlights the importance of the nitrogen atom position in the tricyclic core was written by Kroth, Heiko;Oden, Felix;Serra, Andreia Monica;Molette, Jerome;Mueller, Andre;Berndt, Mathias;Capotosti, Francesca;Gabellieri, Emanuele;Schmitt-Willich, Heribert;Hickman, David;Pfeifer, Andrea;Dinkelborg, Ludger;Stephens, Andrew. And the article was included in Bioorganic & Medicinal Chemistry in 2021.Reference of 76-83-5 This article mentions the following:
Tau aggregates represent a critical pathol. in Alzheimers disease (AD) and other forms of dementia. The extent of Tau neurofibrillary tangles across defined brain regions corresponds well to the observed level of cognitive decline in AD. Compound 1 (PI-2620) was recently identified as a promising Tau positron emission tomog. tracer for AD and non-AD tauopathies. To evaluate the impact of the N-atom position with respect to Tau- and off-target binding, tricyclic core analogs of PI-2620 with nitrogen atoms at different positions were prepared Affinity to aggregated Tau was evaluated using human AD brain homogenates, and their off-target binding was evaluated in a monoamine oxidase A (MAO-A) competition assay. The novel tricyclic core derivatives all displayed inferior Tau binding or MAO-A off-target selectivity, indicating PI-2620 to be the optimal design for high affinity binding to Tau and high MAO-A selectivity. In the experiment, the researchers used many compounds, for example, (Chloromethanetriyl)tribenzene (cas: 76-83-5Reference of 76-83-5).
(Chloromethanetriyl)tribenzene (cas: 76-83-5) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Reference of 76-83-5
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics