20258-98-4Relevant academic research and scientific papers
Construction of Highly Functionalized Xanthones via Rh-Catalyzed Cascade C-H Activation/ O-Annulation
Nale, Sagar D.,Maiti, Debabrata,Lee, Yong Rok
supporting information, p. 2465 - 2470 (2021/04/05)
A facile and efficient strategy for obtaining functionalized and multihydroxylated xanthones via Rh catalysis under redox-neutral conditions is developed. Diverse salicylaldehydes bearing heterocycles, aromatics, and fused aromatics can be rapidly coupled with 1,4-benzoquinones or 1,4-hydroquinones to afford valuable xanthones via cascade C-H/O-H functionalization and annulation. This protocol provides a rapid synthetic approach to obtain biologically active materials through late-stage functionalization and prepares natural products such as subelliptenone, pruniflorone N, and ravenelin.
SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX
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Paragraph 00164, (2020/12/29)
Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.
Discovery of boron-containing compounds as Aβ aggregation inhibitors and antioxidants for the treatment of Alzheimer's disease
Lu, Chuan-Jun,Hu, Jinhui,Wang, Zechen,Xie, Shishun,Pan, Tingting,Huang, Ling,Li, Xingshu
, p. 1862 - 1870 (2018/11/24)
A novel series of boron-containing compounds were designed, synthesized and evaluated as multi-target-directed ligands against Alzheimer's disease. The biological activity results demonstrated that these compounds possessed a significant ability to inhibit self-induced Aβ aggregation (20.5-82.8%, 20 μM) and to act as potential antioxidants (oxygen radical absorbance capacity assay using fluorescein (ORAC-FL) values of 2.70-5.87). In particular, compound 17h is a potential lead compound for AD therapy (IC50 = 3.41 μM for self-induced Aβ aggregation; ORAC-FL value = 4.55). Compound 17h also functions as a metal chelator. These results indicated that boron-containing compounds could be new structural scaffolds for the treatment of AD.
Benzo-hexatomic ring derivative used as DPP-4 inhibitor and application of benzo-hexatomic ring derivative
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Paragraph 0184; 0188; 0189, (2016/10/09)
The invention relates to a benzo-hexatomic ring derivative used as a DPP-4 inhibitor and application of the benzo-hexatomic ring derivative, in particular to compounds shown as in formula I, medicine compositions with the compounds shown as in the formula I and application of the compounds in preparing medicines for treating diseases related to DPP-4 or inhibiting the DPP-4.
Experimental and theoretical studies on constitutional isomers of 2, 6-dihydroxynaphthalene carbaldehydes. effects of resonance-assisted hydrogen bonding on the electronic absorption spectra
Houjou, Hirohiko,Motoyama, Takatoshi,Banno, Seisaku,Yoshikawa, Isao,Araki, Koji
experimental part, p. 520 - 529 (2009/05/30)
We prepared and characterized a series of mono-and dicarbaldehydes of 2, 6-dihydroxynaphthalene that bear potential resonance-assisted hydrogen bonding (RAHB) unit(s). X-ray crystal structures of selected compounds revealed that each salicylaldehyde moiety forms an intramolecular hydrogen bond and that the introduction of formyl groups into either the α-or β-position causes a considerable difference in geometry, which was interpretative from a conventional scheme of resonance hybrids including ionic state. Analyses on NMR chemical shifts suggested that the compounds in solution are present as an equilibrium mixture between closed and open forms with respect to RAHB units. Ab initio calculations indicated that the formation of an intramolecular hydrogen bond strikingly influences the aromaticity of the individual local six-membered ring of naphthalene. The trend of the change in aromaticity was analyzed in connection with the extra stabilization energy of RAHB. In the UV-vis spectra, the β-formyl derivatives specifically showed a substantial red shift compared to α-formyl derivatives. The absorption features were successfully reproduced by TD-DFT calculation, and those data were consistently explained from the effects of RAHB on electronic state of the naphthalene's π-system. Finally, we pointed out a similarity in the electronic state between RAHB-bearing molecules and cata-condensed aromatic hydrocarbons. Copyright 2009 by the American Chemical Society.
Selective irreversible inhibition of fructose 1,6-bisphosphate aldolase from Trypanosoma brucei
Dax, Chantal,Duffieux, Francis,Chabot, Nicolas,Coincon, Mathieu,Sygusch, Jurgen,Michels, Paul A. M.,Blonski, Casimir
, p. 1499 - 1502 (2007/10/03)
An irreversible competitive inhibitor hydroxynaphthaldehyde phosphate was synthesized that is highly selective against the glycolytic enzyme fructose 1,6-bisphosphate aldolase from Trypanosoma brucei (causative agent of sleeping sickness). Inhibition invo
Inhibitors of protein kinase for the treatment of disease
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, (2008/06/13)
The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.
