16738-06-0Relevant articles and documents
ROLES OF MODULATORS OF INTERSECTIN-CDC42 SIGNALING IN ALZHEIMER'S DISEASE
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Paragraph 0272; 0275, (2019/04/14)
Methods of treating Alzheimer's disease and other neurodegenerative and/or neurocognitive and/or neurodevelopmental diseases are described. The methods comprise the administration of compounds that modulate an activity of cell division control protein 42 (Cdc42), such as the interaction between Cdc42 and intersectin (ITSN). Exemplary modulator compounds include thioureas, disulfonamides of fused aromatic systems (e.g., benzofuran), and acyl hydrazones, among others. Some of the modulator compounds act as activators of Cdc42, while others act as inhibitors. In some cases, the modulator compound has dual functionality and the ability of the modulator compound to act as an inhibitor or activator depends on whether or not Cdc42 is already activated in a particular disease stage or biological environment by an upstream activating signal of Cdc42.
Synthesis and biological evaluation of aryloxyacetamide derivatives as neuroprotective agents
Zhong, Yan,Xu, Yi,Zhang, Ai-Xia,Li, Xiao-Feng,Xu, Zhao-Ying,Li, Ping,Wu, Bin
, p. 2526 - 2530 (2016/07/07)
A series of new aryloxyacetamide derivatives 10a-s and 14a-m are designed and synthesized. Their protective activities against the glutamate-induced cell death were investigated in differentiated rat pheochromocytoma cells (PC12 cells). Most compounds exhibited neuroprotective effects, especially for 10m, 10r, 14b and 14c, which showed potential protection of PC12 cells at three doses (0.1, 1.0, 10 μM). MTT assay, Hoechst 33342/PI double staining, and high content screening (HCS) revealed that pretreatment of the cells with 10m, 10r, 14b and 14c has significantly decreased the extent of cell apoptosis in a dose-dependent manner. The results of western blot analysis demonstrated these compounds suppressed apoptosis of glutamate-induced PC12 cells via caspase-3 pathway. These compounds can be lead compounds for further discovery of neuroprotective agents for treating cerebral ischemic stroke. Basic structure-activity relationships are also presented.
Synthesis, structure and biological activities of novel triazole compounds containing Ester Group
Yang, Shuang-Hua,Zhai, Zhi-Wei,Zhang, Shao-Wen
, p. 883 - 886 (2014/06/09)
Novel triazole compounds containing ester group were synthesized. Their structure were confirmed by means of IR, 1H NMR and elemental analysis. The single crystal structure of compound (1H-1,2,4-triazol-1-yl)methyl 3-(2,4-dichlorophenyl)propanoate (compound 3c) was determined via X-ray diffraction. It crystallizes in a monoclinic system with space group P2(1)/c, a = 1.0814(2) nm, b = 0.64514(13) nm, c = 1.8698(4) nm, β = 101.05(3)°, Z = 4, V = 1.2802(5) nm3, Dc = 1.557 Mg/m3, μ = 0.508 mm-1, F(000) = 616 and final R1 = 0.0700. Intermolecular hydrogen-bond and φ-φ stacking interactions exit in the lattice, facilitating the stabilization of crystal structure. The results of the biological test show that these compounds have some fungicidal activity.