1273258-11-9Relevant academic research and scientific papers
Concise synthesis and applications of enantiopure spirobiphenoxasilin-diol and its related chiral ligands
Liu, Tao,Wang, Biqin,Wang, Peng,Wu, Yichen,Xu, Wen-Qiang,Yang, Lei
supporting information, p. 13365 - 13368 (2021/12/17)
The development of chiral architectures for chiral ligand and catalyst discovery is essential for asymmetric catalysis. Herein, we report the concise synthesis of a Si-centered spirocyclic skeleton, spirobiphenoxasilin-diol (SPOSiOL), and its derived chiral ligands. Using the chemical resolution method, the optical SPOSiOL could be obtained in high yield on a gram scale. Preliminary studies indicated that this ligand scaffold has great potential in transition metal-catalyzed asymmetric reactions. This finding further highlights that the Si-centered spirocyclic scaffolds are of great value in asymmetric catalysis. This journal is
Compounds serving as BACE1 inhibitors and application thereof
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Paragraph 0218; 0220-0222, (2020/04/17)
The invention belongs to the field of medical chemistry and relates to compounds serving as BACE1 inhibitors and application of the compounds. Specifically, the invention provides the compounds as shown in a formula I which is described in the specification or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, a preparation method of the compounds, pharmaceutical compositions containing the compounds and application of the compounds or the compositions to treatment and/or prevention of BACE1 related diseases, such as Alzheimer's disease, Huntington's disease, Down's syndrome, beta-like amyloid vascular disease and the like. The compounds provided by the invention show very good inhibitory activity on hBACE1 enzyme, has lower inhibitory activity on hCathepsin D enzyme, is high in selectivity, and is very expected to become a therapeutic agent for BACE1 related diseases and with higher curative effect and smaller side effects.
An Atropos Chiral Biphenyl Bisphosphine Ligand Bearing Only 2,2′-Substituents and Its Application in Rh-Catalyzed Asymmetric Hydrogenation
Jia, Jia,Ling, Zheng,Zhang, Zhenfeng,Tamura, Ken,Gridnev, Ilya D.,Imamoto, Tsuneo,Zhang, Wanbin
supporting information, p. 738 - 743 (2017/12/26)
An atropos chiral biphenyl bisphosphine ligand bearing only 2,2′-substituents was rationally designed and easily synthesized utilizing a bulky chiral t-butylmethylphosphino block. Computational results showed a large difference in the free energies betwee
Green fluorescent protein chromophore derivatives as a new class of aldose reductase inhibitors
Saito, Ryota,Hoshi, Maiko,Kato, Akihiro,Ishikawa, Chikako,Komatsu, Toshiya
, p. 965 - 974 (2016/10/25)
A number of (Z)-4-arylmethylene-1H-imidazol-5(4H)-ones, which are related to the fluorescent chromophore of the Aequorea green fluorescent protein (GFP), have been synthesized and evaluated their in vitro inhibitory activity against recombinant human aldo
ANTIDIABETIC ENOLIC GLUCOSIDE OF PHENYLPYRUVIC ACID
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Paragraph 0207; 0208; 0209, (2016/10/07)
PROBLEM TO BE SOLVED: To provide an antidiabetic enolic glucoside of phenylpyruvic acid and derivatives thereof, for use as medicaments, especially normoglycemic agents, i.e. for lowering blood glucose levels to normal levels in mammals that are obese, pr
Synthesis of new simplified hemiasterlin derivatives with α,β-unsaturated carbonyl moiety
The, Chinh Pham,Thi, Tuyet Anh Dang,Hoang, Thi Phuong,Ngo, Quoc Anh,Doan, Duy Tien,Thi, Thu Ha Nguyen,Thi, Tham Pham,Thi, Thu Ha Vu,Jean,Van De Weghe,Van, Tuyen Nguyen
supporting information, p. 2244 - 2246 (2014/05/20)
In this Letter, we report a convenient and efficient method for the synthesis of new simplified derivatives of hemiasterlin in which the α,α-dimethylbenzylic moiety A is replaced by α,β- unsaturated aryl groups as Michael acceptor. Most of these derivatives have a strong cytotoxic activity on three human tumor cell lines (KB, Hep-G2 and MCF7). Analogs 17b and 17f showed a high cytotoxicity against KB and Hep-G2 cancer cell lines comparable to paclitaxel and ellipticine.
Oxazolone-based photoswitches: Synthesis and properties
Blanco-Lomas, Marina,Funes-Ardoiz, Ignacio,Campos, Pedro J.,Sampedro, Diego
supporting information, p. 6611 - 6618 (2013/11/06)
The synthesis, photophysics and photochemistry of a family of molecular switches inspired by the green fluorescent protein (GFP) chromophore is presented. These compounds can be synthesized in one step and good yields, their photophysical properties may b
Benzylidene-oxazolones as photoswitches: Photochemistry and theoretical calculations
Funes-Ardoiz, Ignacio,Blanco-Lomas, Marina,Campos, Pedro J.,Sampedro, Diego
supporting information, p. 9766 - 9771 (2013/10/22)
The photophysics and photochemistry of a family of compounds proposed as efficient molecular photoswitches is presented. The effect of different light sources, substituents and solvents in the photostationary state has been explored. A detailed mechanisti
Synthesis of novel cinnamanilides as potential immunosuppressive agents
Shi, Lei,Wang, Lu,Wang, Zhi,Zhu, Hai-Liang,Song, Qiao
experimental part, p. 585 - 593 (2012/02/14)
A series of new cinnamanilides (6-40) were synthesized and their immunosuppressive activity and cytotoxicity were evaluated. Most of the cinnamanilides showed good immunosuppressive activity. Among the synthesized compounds, (Z)-N-(4-bromophenyl)-2-methox
Pseudo-peptides derived from isomannide: Inhibitors of serine proteases
Barros, Thalita G.,Pinheiro, Sergio,Williamson,Tanuri, Amilcar,Gomes Jr.,Pereira, Helena S.,Brindeiro,Neto, Jose B. A.,Antunes,Muri, Estela M. F.
scheme or table, p. 701 - 709 (2010/08/05)
In this paper, we describe the synthesis of a novel class of pseudo-peptides derived from isomannide and several oxazolones as potential inhibitors of serine proteases as well as preliminary pharmacological assays for hepatitis C. Hepatitis C, dengue and West Nile fever are among the most important flaviviruses that share one important serine protease enzyme. Serine proteases belong to the most studied class of proteolytic enzymes and are a primary target in the drug development field. Several pseudo-peptides were obtained in good yields from the reaction of isomannide and oxazolones, and their anti-HCV potential using the HCV replicon-based assay was shown.
