3652-90-2Relevant 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 (2019/01/24)
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.
Organic metal compounds and organic light emitting diodes comprising the same
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Paragraph 0269; 0276; 0278-0281, (2018/10/19)
PURPOSE: An organic metal compound and an organic electroluminescent device containing the same are provided to ensure excellent thermal property and luminescence efficiency, and to be used in a display and a light. CONSTITUTION: An organic metal compound contains a compound of chemical formula 1. An organic electroluminescent device contains the organic metal compound of chemical formula 1. The compound is contained in a light emitting layer between anode and cathode. The organic electroluminescent device comprises one or more layers selected from a hole injection layer, a hole transport layer, an electron blocking layer, a hole blocking layer, an electron transport layer, and an electron injection layer between the anode and the cathode.
Blue light emission of new anthracene derivatives produced using optimized side group link positions
Kang, Seokwoo,Jung, Hyocheol,Lee, Hayoon,Lee, Suji,Jung, Mina,Lee, Jaehyun,Chul Kim, Young,Park, Jongwook
, p. 369 - 378 (2018/05/09)
Using an anthracene chromophore as a core group and a phenyl carbazole chromophore as a side group, three new emitters of blue light, 2-DCPA, 3-DCPA and 4-DCPA, were synthesized. The three compounds differed with regard to the position of the carbazole linked to the core, with 2-DCPA and 4-DCPA using carbazole nodes and 3-DCPA using the lobe position. Density functional theory calculations were performed to determine which positions of the carbazole moiety had node characteristics and which had lobe characteristics. The PLmax values of 2-DCPA, 3-DCPA and 4-DCPA in the film state were in the blue region, at 453, 457, and 452 nm, respectively. Of these materials, 3-DCPA, i.e., that with the linkage to the lobe position, showed the highest efficiency, with a value of 2.91 cd/A, and EQE, with a value of 2.65%. In a doped device using CBP as a host material and 3-DCPA as a dopant, the ELmax emission was observed to be in the deep blue region, at 433 nm, and with a CIE value of (0.150, 0.068).
