111600-85-2Relevant academic research and scientific papers
Synthesis and anti-inflammatory activity of ethynylthiazoles
Geronikaki,Vasilevsky,Hadjipavlou-Litina,Lagunin,Poroikov
, p. 675 - 680 (2006)
A series of acetylene derivatives of thiazole using the Sonogashira cross-coupling method was synthesized and evaluated in vivo for their anti-inflammatory activity. Four compounds exhibited good anti-inflammatory activity and two inhibited soybean lipoxy
TETRAHYDROPYRAN-BASED THIODISACCHARIDE MIMICS AS GALECTIN-3 INHIBITORS
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Page/Page column 26, (2020/01/08)
The present disclosure relates to compounds of Formula (1), which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods making and using such compounds and compositions.
Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors
Keeley,ábrányi-Balogh,Keseru
supporting information, p. 263 - 267 (2019/03/05)
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads. The analysis of theoretical and experimental descriptors revealed correlations between the electronic properties of the heterocyclic cores and their reactivity against GSH that are helpful in identifying suitable fragments for cysteines with specific nucleophilicity. The most important advantage of these fragments is that they show only minimal structural differences from non-electrophilic counterparts. Therefore, they could be used effectively in the design of targeted covalent inhibitors with minimal influence on key non-covalent interactions.
Design and synthesis of O-GlcNAcase inhibitors via 'click chemistry' and biological evaluations
Li, Tiehai,Guo, Lina,Zhang, Yan,Wang, Jiajia,Li, Zhonghua,Lin, Lin,Zhang, Zhenxing,Li, Lei,Lin, Jianping,Zhao, Wei,Li, Jing,Wang, Peng George
experimental part, p. 1083 - 1092 (2011/06/22)
Protein O-GlcNAcylation has been shown to play an important role in a number of biological processes, including regulation of the cell cycle, DNA transcription and translation, signal transduction, and protein degradation. O-GlcNAcase (OGA) is responsible for the removal of O-linked β-N-acetylglucosamine (O-GlcNAc) from serine or threonine residues, and thus plays a key role in O-GlcNAc metabolism. Potent OGA inhibitors are useful tools for studying the cellular processes of O-GlcNAc, and may be developed as drugs for the treatment neurodegenerative diseases. In this study, Cu(I)-catalyzed 'Click' cycloaddition reactions between glycosyl azides and alkynes were exploited to generate inhibitory candidates of OGA. Enzymatic kinetic screening revealed that compound 7 was a potent competitive inhibitor of human O-GlcNAcase (Ki = 185.6 μM). Molecular docking simulations of compound 7 into CpOGA (Clostridium perfringens OGA) suggested that strong π-π stacking interaction between the compound and W490 considerably contributed to improving the inhibitory activity. Crown Copyright
(DIHYDRO)PYRROLO[2,1-A]ISOQUINOLINES
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Page/Page column 79, (2009/10/09)
The invention relates to 5,6 - dihydropyrrolo [2,1-a] isoquinoline and pyrrolo[2,1-a] isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
2-CARBOXY THIOPHENE DERIVATIVES AS ANTI-VIRAL AGENTS
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Page/Page column 33, (2008/12/08)
Anti-viral agents of compounds of Formula (I) : wherein A, Rx, Ry, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.
Heterotopic Assemblage of Two Different Disk-Shaped Ligands through Trinuclear Silver(I) Complexation: Ligand Exchange-Driven Molecular Motion
Hiraoka, Shuichi,Shiro, Motoo,Shionoya, Mitsuhiko
, p. 1214 - 1218 (2007/10/03)
The sandwich-shaped heterotopic trinuclear Ag+ complex Ag 31·2 was exclusively formed from two different tris(thiazolyl) and hexa(thiazolyl) disk-shaped ligands, 1 and 2, with the aid of three Ag + ions. The variable-temperature 1H NMR study on its complexation behavior revealed that metal-ligand exchanges between the two neighboring thiazolyl nitrogen donors of 2 take place at the three Ag + centers in concert. ΔH? and ΔS? for the exchange process were calculated to be 50.5 kJ mol-1 and -26.7 J mol-1 K-1, respectively, and its energy barrier at 298 K was estimated to be 58.5 kJ mol-1. Each concerted metal-ligand exchange leads to an intramolecular 60°-rotational motion ((P) ? (M) conversion) between the two disk-shaped ligands.
Synthesis of High Carbon Materials from Acetylenic Precursors. Preparation of Aromatic Monomers Bearing Multiple Ethynyl Groups
Neenan, Thomas X.,Whitesides, George M.
, p. 2489 - 2496 (2007/10/02)
The synthesis of polyethynyl aromatics as starting materials for the preparation of highly cross-linked organic solids containing high atom fractions of carbon is described.Treatment of bromo- and iodoaromatic compounds with (trimethylsilyl)acetylene (TMSA) in the presence of palladium(O) and copper(I) in amine solvents yields (trimethylsilyl)ethynyl-substituted aromatics.The TMS protecting groups can be removed by hydrolysis with mild base.Compounds prepared by using this technique include 1,3-diethynylbenzene, 2,5-diethynylthiophene, 1,3-diethynyltetrafluorobenzene, 1,4-diethynyltetrafluorobenzene, 2-ethynylthiazole, 2,4-diethynylthiazole, 2,7-diethynylnaphthalene, hexakis((trimethylsilyl)ethynyl)benzene, tetraethynylthiophene, 2,5-bis((trimethylsilyl)ethynyl)-3,4-bis(3-hydroxy-3-methyl-1-butynyl)thiophene, 2,5-diethynyl-3,4-bis(3-hydroxy-3-methyl-1-butynyl)thiophene, 2,5-bis(4-(2-thienyl)butadiynyl)-3,4-bis(3-hydroxy-3-methyl-1-butynyl)thiophene, and 2,5-bis-(4-(2-thienyl)butadiynyl)-3,4-diethynylthiophene.
