25829-00-9Relevant academic research and scientific papers
Enantioselective synthesis and anti-parasitic properties of aporphine natural products
Amaral, Maiara,Anderson, Edward A.,McHugh, Eliza,Pieper, Pauline,Tempone, Andre G.
, (2019)
Chagas disease and visceral leishmaniasis are neglected protozoan diseases with significant impact in developing countries. Due to the limited number and toxicity of current therapies, new drug leads are urgently needed. In this work, four aporphine natural products were synthesized using an enantioselective, modular and convergent strategy, comprising eight steps in the longest linear sequence; key steps included Bischler-Napieralski cyclization/Noyori asymmetric reduction to construct the tetrahydroisoquinolines, and palladium-catalyzed arylation to close the C ring. Norglaucine, nordicentrine and dicentrine showed promising bioactivity against T. cruzi and L. infantum, suggesting potential for further development of these scaffolds as antiparasitic agents.
Oxidized dicentra spectabilis alkali rare earth compound as well as synthesis method and application thereof
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Paragraph 0025; 0031-0033, (2019/02/25)
The invention discloses an oxidized dicentra spectabilis alkali rare earth compound as well as a synthesis method and application thereof. The rare earth compound is obtained by dissolving oxidized dicentra spectabilis alkali and rare earth metal salt int
Bromated oxidated dicentrine and synthesis method and application thereof
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Paragraph 0048; 0052-0054, (2019/04/04)
The invention discloses bromated oxidated dicentrine and a synthesis method and application thereof. The synthesis method of the bromated oxidated dicentrine comprises the steps of subjecting 3,4-dimethoxyphenylacetic acid, which serves as a starting raw
In order to bromo ligand dutch bud peony alkali oxide of the rare earth complex and its synthetic method and application (by machine translation)
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Paragraph 0063-0065, (2019/05/08)
The invention discloses a dutch bud peony alkali as ligand to bromo oxidation of the rare earth complex and its synthetic method and application. The rare earth complex is to bromo dutch bud peony alkali oxide and a rare earth metal salt in the solvent sy
In vitro functional evaluation of isolaureline, dicentrine and glaucine enantiomers at 5-HT2 and α1 receptors
Heng, Hui Li,Chee, Chin Fei,Thy, Chun Keng,Tee, Jia Ti,Chin, Sek Peng,Herr, Deron R.,Buckle, Michael J. C.,Paterson, Ian C.,Doughty, Stephen W.,Abd. Rahman, Noorsaadah,Chung, Lip Yong
, p. 132 - 138 (2018/10/15)
Compounds with activity at serotonin (5-hydroxytryptamine) 5-HT2 and α1 adrenergic receptors have potential for the treatment of central nervous system disorders, drug addiction or overdose. Isolaureline, dicentrine and glaucine enantiomers were synthesized, and their in vitro functional activities at human 5-HT2 and adrenergic α1 receptor subtypes were evaluated. The enantiomers of isolaureline and dicentrine acted as antagonists at 5-HT2 and α1 receptors with (R)-isolaureline showing the greatest potency (pKb?=?8.14 at the 5-HT2C receptor). Both (R)- and (S)-glaucine also antagonized α1 receptors, but they behaved very differently to the other compounds at 5-HT2 receptors: (S)-glaucine acted as a partial agonist at all three 5-HT2 receptor subtypes, whereas (R)-glaucine appeared to act as a positive allosteric modulator at the 5-HT2A receptor.
Synthesizing method of oxidized dicentrine
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Paragraph 0042; 0046-0048, (2019/03/28)
The invention discloses a synthesizing method of oxidized dicentrine. The synthesizing method comprises the following steps of using 3,4-dimethoxyphenylacetic acid as the start raw material, reactingwith bromine to obtain a product, and then reacting with
