3306-62-5Relevant articles and documents
INHIBITORS OF PHOSPHOLIPID SYNTHESIS AND METHODS OF USE
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Page/Page column 92, (2021/02/26)
Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome, hyperlipidemia, infection and inflammation.
Easy preparation of novel 3,3-dimethyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide: Molecular structure, Hirshfeld surface, NCI analyses and molecular docking on AMPA receptors
Etsè, Koffi Sénam,Zaragoza, Guillermo,Etsè, Kodjo Djidjolé
, (2021/04/27)
We present in this study the synthesis and characterization of a new 3,3-dimethyl-substituted 1,2,4-benzothiadiazine 1,1-dioxide. 3,3-dimethyl-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide 10, was obtained by reacting 2-aminobenzenesulfonamide with acetone. The molecular structures of the starting sulfonamide and the new benzothiadiazine were obtained by X-ray diffraction analysis and the interactions like hydrogen bonds stabilizing the crystal packing were discussed. The contacts are confirmed by non-covalent interaction analysis. Analyses of Hirshfeld surface mapped over di, de, dnorm and shape-index were further used to identify the intermolecular interactions. The fingerprint histogram allow to show that H···H (45.7%) and O···H (30.1%) contacts are the dominant interactions in the crystal packing of 10. The effects of the molecular environment were accessed by analyzing the electron density isosurface and the 3D-topology of energy frameworks. The prediction of physicochemical properties suggested that 10 could be considered as a lead-like drug. Therefore, molecular docking study was performed on the α-amino-3?hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) and suggested that 10 could interact with the allosteric site located on the ligand binding domain of AMPAR and could be a positive allosteric modulator. Docking results show that 10 can bind in a symmetrical way in the GluA2 ligand binding domain with two molecules at the dimer interface. The results also demonstrated that the presence of two methyl groups at the 3-position of the thiadiazine ring induced rotation of 10 in the binding site leading to close contacts with Pro494, Ser497, Ser729 and Ser754.
Benzothiadiazine methoxy acrylate derivatives and preparation method and application thereof
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Paragraph 0023-0025, (2020/07/24)
The invention provides benzothiadiazine methoxy acrylate derivatives and a preparation method and application thereof, and the benzothiadiazine methoxy acrylate derivatives have the following chemicalstructural general formula VII as shown in the description, wherein R1 is hydrogen, fluorine, chlorine, bromine, iodine, methyl, ethyl, methoxy or nitro; and R2 is hydrogen, methyl or benzyl. According to the invention, an active group 3, 4-dihydro-2H-1, 2, 4-benzothiadiazine-1, 1-dioxo substitutes the side chain part of the methoxy acrylate bactericide and then is reasonably spliced with the pharmacophore of the methoxy acrylate bactericide, so that the bactericide with novel structure, broad spectrum, high efficiency and low toxicity is synthesized, the bactericide can be alternately used with the existing bactericide, the generation of resistance is avoided or delayed, the preparation conditions are conventional, the subsequent treatment is simple and convenient, and the industrialization is easy to realize.
FUSED [1,2,4]THIADIAZINE DERIVATIVES WHICH ACT AS KAT INHIBITORS OF THE MYST FAMILY
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Page/Page column 51, (2019/03/17)
A compound of formula (I): which inhibits the activity of one or more KATs of the MYST family, i.e., TIP60, KAT6B, MOZ, HBO1 and MOF.
MYELINATION STIMULATOR COMPOUNDS, AND METHODS OF TREATMENT
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Page/Page column 27, (2019/11/28)
The invention is directed towards compounds, methods of stimulating myelination, stimulating proliferation of oligodendrocytes (OLs) or stimulating oligodendrocyte precursor cells and methods of treating diseases, disorders or symptoms thereof.
Iridium-Catalyzed ortho-C?H Amidation of Benzenesulfonamides with Sulfonyl Azides
Hou, Hongcen,Zhao, Yongli,Sheng, Shouri,Chen, Junmin
, p. 4393 - 4398 (2019/08/28)
We developed herein an iridium-catalyzed direct C?H activation/ C?N bond formation reaction of benzenesulfonamides with sulfonyl azides. The amidation reaction provides a protocol for the synthesis of 2-aminobenzesulfonamides in good to excellent yields. This strategy features a wide substrate scope, tolerates a broad range of functional groups under external oxidant-free conditions and only releases molecular nitrogen as the sole by-product. Moreover, the preliminary mechanism was investigated and the proposed reaction pathway was provided. (Figure presented.).
Cobalt-based nanoparticles prepared from MOF-carbon templates as efficient hydrogenation catalysts
Murugesan, Kathiravan,Senthamarai, Thirusangumurugan,Sohail, Manzar,Alshammari, Ahmad S.,Pohl, Marga-Martina,Beller, Matthias,Jagadeesh, Rajenahally V.
, p. 8553 - 8560 (2018/11/30)
The development of efficient and selective nanostructured catalysts for industrially relevant hydrogenation reactions continues to be an actual goal of chemical research. In particular, the hydrogenation of nitriles and nitroarenes is of importance for the production of primary amines, which constitute essential feedstocks and key intermediates for advanced chemicals, life science molecules and materials. Herein, we report the preparation of graphene shell encapsulated Co3O4- and Co-nanoparticles supported on carbon by the template synthesis of cobalt-terephthalic acid MOF on carbon and subsequent pyrolysis. The resulting nanoparticles create stable and reusable catalysts for selective hydrogenation of functionalized and structurally diverse aromatic, heterocyclic and aliphatic nitriles, and as well as nitro compounds to primary amines (>65 examples). The synthetic and practical utility of this novel non-noble metal-based hydrogenation protocol is demonstrated by upscaling several reactions to multigram-scale and recycling of the catalyst.
Highly chemoselective reduction of nitroarenes over non-noble metal nickel-molybdenum oxide catalysts
Huang, Haigen,Wang, Xueguang,Li, Xu,Chen, Chenju,Zou, Xiujing,Ding, Weizhong,Lu, Xionggang
, p. 809 - 815 (2017/08/15)
The chemoselective reduction of nitroarenes is an important transformation for the production of arylamines, which are the primary intermediates in the synthesis of pharmaceuticals, agrochemicals and dyes. Heterogeneous non-noble metal nickel-molybdenum oxide catalysts supported on ordered mesoporous silica SBA-15 (Ni-MoO3/CN@SBA-15) were prepared for the first time by treating SBA-15-supported nickel-molybdenum oxide materials with 1,10-phenanthroline, and exhibited unprecedented catalytic activity and chemoselectivity for the reduction of various substituted nitroarenes to the corresponding aromatic amines in ethanol with hydrazine hydrate as a hydrogen donor under mild conditions owing to the synergistic effect of metal Ni and MoO3 species, affording excellent yields of >99% within very short reaction periods (≤60 min). The Ni-MoO3/CN@SBA-15 catalysts were highly stable and could easily be recovered by simple filtration or by an external magnetic field for at least ten recycling reactions without any observable loss of catalytic performance or leaching of metal components.
Benzothiadiazine derivatives as well as preparation method and application thereof
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Paragraph 0099; 0100; 0101, (2017/12/28)
The invention discloses benzothiadiazine derivatives as well as preparation methods and application thereof. The compounds have the structures of formula I or II. The invention also relates to preparation methods of the compounds containing the structures of formula I or II, pharmaceutical compositions and the application of the compounds in the preparation of anti-HBV drugs. The formula I or II are shown in the description.
1. 1 - dioxo - 4H - benzo [1, 2, 4] - thiadiazine hydrochloric acid salt compound and its preparation method
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Paragraph 0028-0030, (2017/03/08)
The invention discloses a 1,1-dioxo-4H-benzo[1,2,4]-thiadiazine hydrochloride compound and a preparation method thereof, belonging to the technical field of organic synthesis. The technical scheme has the key point as follows: the 1,1-dioxo-4H-benzo[1,2,4]- thiadiazine hydrochloride compound has the structure as shown in the specification, wherein R is H, -CH3 or -C2H5. The invention also discloses the preparation method of the 1,1-dioxo-4H-benzo[1,2,4]-thiadiazine hydrochloride compound. The preparation method is simple, convenient and easy to operate, relatively high in reaction efficiency and relatively good in repeatability, and raw materials are cheap and available.
