82072-22-8Relevant articles and documents
Galantamine-curcumin hybrids as dual-site binding acetylcholinesterase inhibitors
Atanasova, Mariyana,Atanasova, Teodora,Doytchinova, Irini,Ivanov, Stefan,Konstantinov, Spiro,Lukarski, Atanas,Philipova, Irena,Stavrakov, Georgi,Zheleva, Dimitrina,Zhivkova, Zvetanka D.
supporting information, (2020/08/06)
Galantamine (GAL) and curcumin (CU) are alkaloids used to improve symptomatically neurodegenerative conditions like Alzheimer's disease (AD). GAL acts mainly as an inhibitor of the enzyme acetylcholinesterase (AChE). CU binds to amyloid-beta (Aβ) oligomers and inhibits the formation of Aβ plaques. Here, we combine GAL core with CU fragments and design a combinatorial library of GAL-CU hybrids as dual-site binding AChE inhibitors. The designed hybrids are screened for optimal ADME properties and BBB permeability and docked on AChE. The 14 best performing compounds are synthesized and tested in vitro for neurotoxicity and anti-AChE activity. Five of them are less toxic than GAL and CU and show activities between 41 and 186 times higher than GAL.
Aromatic PCN palladium pincer complexes. Probing the hemilability through reactions with nucleophiles
Fleckhaus, André,Mousa, Abdelrazek H.,Lawal, Nasir Sallau,Kazemifar, Nitsa Kiriakidou,Wendt, Ola F.
, p. 1627 - 1634 (2015/05/20)
A series of unsymmetrical PCN pincer ligands (1-(3-((di-tert-butylphosphino)methyl)phenyl)-N,N-dialkylmethanamine) were cyclometalated with palladium to generate a series of new PCN supported Pd(II) chloro complexes, (PCN)PdCl (4-6), where alkyl = methyl, ethyl, and n-propyl, which were fully characterized by NMR spectroscopy and X-ray crystallography. The N,N-dimethyl complex 4 reacts with methyl lithium to give the corresponding methyl and dimethyl complexes (PCN)PdMe (12) and Li[(PCN)PdMe2] (13), which could not be isolated but were characterized in solution. The substitution reactions of (PCN)PdCl (4-6) with iodide to form the corresponding iodo complexes (PCN)PdI (7-9) were investigated by use of UV-vis stopped-flow spectrophotometry. The experiments were performed in methanol over a temperature range from 293 to 325 K. The reactions are reversible and were shown to proceed exclusively via the solvento complex in two reversible consecutive steps. Activation parameters for both the forward and reverse reactions were determined, and they, together with reactivity trends, support an associative pathway. No displacement of the nitrogen donor was detected, and overall this points to a limited hemilability of the ligands on palladium.
PIPERIDINE-DIONE DERIVATIVES
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Page/Page column 106, (2015/11/10)
The invention provides novel compounds having the general formula (I) and tautomers and pharmaceutically acceptable salts thereof, wherein A1, A2, A3, A4, R1, R4, R5, R6, R7 and R8 are as defined herein, compositions including the compounds and methods of using the compounds.