17613-47-7Relevant articles and documents
Design, Synthesis, and Pharmacological Characterization of Carbazole Based Dopamine Agonists as Potential Symptomatic and Neuroprotective Therapeutic Agents for Parkinson's Disease
Elmabruk, Asma,Das, Banibrata,Yedlapudi, Deepthi,Xu, Liping,Antonio, Tamara,Reith, Maarten E. A.,Dutta, Aloke K.
, p. 396 - 411 (2019)
We have developed a series of carbazole-derived compounds based on our hybrid D2/D3 agonist template to design multifunctional compounds for the symptomatic and disease-modifying treatment of Parkinson's disease (PD). The lead molecules (-)-11b (D-636), (-)-15a (D-653), and (-)-15c (D-656) exhibited high affinity for both D2 and D3 receptors and in GTPγS functional assay, the compounds showed potent agonist activity at both D2 and D3 receptors (EC50 (GTPγS); D2 = 48.7 nM, D3 = 0.96 nM for 11b, D2 = 0.87 nM, D3 = 0.23 nM for 15a and D2 = 2.29 nM, D3 = 0.22 nM for 15c). In an animal model of PD, the test compounds exhibited potent in vivo activity in reversing hypolocomotion in reserpinized rats with a long duration of action compared to the reference drug ropinirole. In a cellular antioxidant assay, compounds (-)-11b, (-)-15a, and (-)-15c exhibited potent activity in reducing oxidative stress induced by neurotoxin 6-hydroxydopamine (6-OHDA). Also, in a cell-based PD neuroprotection model, these lead compounds significantly increased cell survival from toxicity of 6-OHDA, thereby producing a neuroprotective effect. Additionally, compounds (-)-11b and (-)-15a inhibited aggregation and reduced toxicity of recombinant alpha synuclein protein in a cell based in vitro assay. These observations suggest that the lead carbazole-based dopamine agonists may be promising multifunctional molecules for a viable symptomatic and disease-modifying therapy of PD and should be further investigated.
Condensed-ring compound and preparation method and application thereof
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Paragraph 0082; 0087-0091; 0388; 0390-0394, (2020/02/10)
The invention discloses a condensed-ring compound and a preparation method and an application thereof. The condensed-ring compound has a structure represented by formula (I) or formula (II). The HOMOand LUMO energy levels of the fused-ring compound are completely separated, so that the energy gap width of the material is reduced, the three-wire energy level is improved, and the energy backflow from the object material to the main material is avoided to reduce the luminous efficiency; HOMO and LUMO energy levels are matched with adjacent materials, and the driving voltage is small. The devicehas large molecular structure size and good intramolecular conjugation, so it has good thermal stability, can avoid thermal decomposition of materials during film formation or use, avoids loss of material layer function, and improves luminous efficiency and luminous performance of the device. The invention also provides a preparation method of the fused-ring compound and its application as an organic electroluminescent material.
Novel anthracene derivatives and organic light-emitting diode therewith
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Paragraph 0319; 0412-0417, (2018/04/12)
The present invention relates to an anthracene derivative represented by chemical formula A, and an organic light-emitting device including the same. In the chemical formula A, R_1- R_10, L, M, and n are the same as defined in the present specification. According to the present invention, the organic light-emitting device including the compound in light-emitting layers exhibits long lifespan and high efficiency compared to existing organic light-emitting devices.COPYRIGHT KIPO 2018