54353-48-9Relevant articles and documents
Design, synthesis and evaluation of pentacycloundecane and hexacycloundecane propargylamine derivatives as multifunctional neuroprotective agents
Zindo, Frank T.,Malan, Sarel F.,Omoruyi, Sylvester I.,Enogieru, Adaze B.,Ekpo, Okobi E.,Joubert, Jacques
, p. 83 - 94 (2019)
The multifactorial pathophysiology of neurodegenerative disorders remains one of the main challenges in the design of a single molecule that may ultimately prevent the progression of these disorders in affected patients. In this article, we report on twelve novel polycyclic amine cage derivatives, synthesized with or without a propargylamine function, designed to possess inherent multifunctional neuroprotective activity. The MTT cytotoxicity assay results showed the SH-SY5Y human neuroblastoma cells to be viable with the twelve compounds, particularly at concentrations less than 10 μM. The compounds also showed significant neuroprotective activity, ranging from 31% to 61% at 1 μM, when assayed on SH-SY5Y human neuroblastoma cells in which neurodegeneration was induced by MPP+. Calcium regulation assays conducted on the same cell line showed the compounds to be significant VGCC blockers with activity ranging from 26.6% to 51.3% at 10 μM; as well as significant NMDAr antagonists with compound 5 showing the best activity of 88.3% at 10 μM. When assayed on human MAO isoenzymes, most of the compounds showed significant inhibitory activity, with compound 5 showing the best activity (MAO-B: IC50 = 1.70 μM). Generally, the compounds were about 3–52 times more selective to the MAO-B isoenzyme than the MAO-A isoenzyme. Based on the time-dependency studies conducted, the compounds can be defined as reversible MAO inhibitors. Several structure activity relationships were derived from the various assays conducted, and the compounds’ possible putative binding modes within the MAO-B enzyme cavity were assessed in silico.
Underwater diene addition reaction synthesizing method and application thereof in synthesizing of double-cage spiro hydrocarbon PCUD
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Paragraph 0047; 0052-0055, (2019/09/17)
The invention provides an underwater diene addition reaction synthesizing method and application thereof in synthesizing of double-cage spiro hydrocarbon PCUD. The synthesizing method is characterizedin that p-benzoquinone and cyclic conjugate diolefins are treated as raw materials, and water is treated as a dispersant, and on that basis, Diels-Alder addition reaction is carried out. According tothe method, pure water is treated as a medium in the reaction; and the reaction post-treatment is simple, and easy to carry out; the energy consumption is low; and the yield is high.
UV PhotoVap: Demonstrating How a Simple and Versatile Reactor Based on a Conventional Rotary Evaporator Can Be Used for UV Photochemistry
Clark, Charlotte A.,Lee, Darren S.,Pickering, Stephen J.,Poliakoff, Martyn,George, Michael W.
supporting information, p. 595 - 599 (2018/08/17)
We report the use of a simple rotary evaporator as a semi-continuous UV photochemical reactor. By generation of a thin film from the rotation of a flask, better light penetration is achieved, and in this work we used high-power Hg lamps to enable the direct irradiation of molecules with UV light. The intramolecular [2 + 2] photocycloaddition of Cookson's dione and the intermolecular [2 + 2] photocycloaddition of maleimide with 1-hexyne were used as test reactions to examine the effectiveness of this reactor. High productivities, equivalent to 210 g h-1, were obtained for the simple intramolecular reaction, demonstrating the scalability of the reactor. The effects of flask size, reaction mixture volume, and use of borosilicate or quartz glassware were also investigated.
