4693-38-3Relevant academic research and scientific papers
Unravelling the potency of triazole analogues for inhibiting α-synuclein fibrillogenesis andin vitrodisaggregation
Maqbool, Mudasir,Gadhavi, Joshna,Singh, Anju,Hivare, Pravin,Gupta, Sharad,Hoda, Nasimul
supporting information, p. 1589 - 1603 (2021/03/01)
A series of triazole-based compounds was synthesized using a click chemistry approach and evaluated for the inhibition of α-synuclein (α-syn) fibrillogenesis and its disaggregation. CompoundsTr3,Tr7,Tr12,Tr15, andTr16exhibited good effect in inhibiting α-
4-Methyltetrahydropyran (4-MeTHP): Application as an Organic Reaction Solvent
Kobayashi, Shoji,Tamura, Tomoki,Yoshimoto, Saki,Kawakami, Takashi,Masuyama, Araki
, p. 3921 - 3937 (2019/11/11)
4-Methyltetrahydropyran (4-MeTHP) is a hydrophobic cyclic ether with potential for industrial applications. We herein report, for the first time, a comprehensive study on the performance of 4-MeTHP as an organic reaction solvent. Its broad application to organic reactions includes radical, Grignard, Wittig, organometallic, halogen-metal exchange, reduction, oxidation, epoxidation, amidation, esterification, metathesis, and other miscellaneous organic reactions. This breadth suggests 4-MeTHP can serve as a substitute for conventional ethers and harmful halogenated solvents. However, 4-MeTHP was found incompatible with strong Lewis acids, and the C?O bond was readily cleaved by treatment with BBr3. Moreover, the radical-based degradation pathways of 4-MeTHP, THP and 2-MeTHF were elucidated on the basis of GC-MS analyses. The data reported herein is anticipated to be useful for a broad range of synthetic chemists, especially industrial process chemists, when selecting the reaction solvent with green chemistry perspectives.
Mechanistic studies of base-catalysed lignin depolymerisation in dimethyl carbonate
Dabral, Saumya,Engel, Julien,Mottweiler, Jakob,Spoehrle, Stephanie S. M.,Lahive, Ciaran W.,Bolm, Carsten
supporting information, p. 170 - 182 (2018/03/21)
The depleting fossil reservoirs have stimulated global research initiatives on renewable lignin feedstocks as sustainable alternatives to petroleum-derived aromatics. Base-catalysed depolymerisation (BCD) is regarded as an economical and efficient approach for the valorisation of technical lignins. The major limiting factor encountered during this process is the re-condensation of the formed phenolic products, which results in lower monomer yields. To diminish these side reactions, we selected alkali earth metal catalysts in dimethyl carbonate (DMC) to produce methylated phenol derivatives as the final products. Herein, we demonstrate for the first time a base-promoted depolymerisation process affording low-molecular weight oils in high yields (52-67 wt%) wherein the employed bases are used in truly catalytic quantities (with catalyst loadings of around 5 mol%). The general applicability of this methodology was proved on four different lignin samples (1 Kraft, 3 organosolv) using caesium carbonate and lithium tert-butoxide as catalysts. The 2D NMR studies on the post-reaction lignin samples showed a similar degradation of the major lignin linkages for both bases. A difference in the reduction of phenolic moieties was revealed by quantitative 31P NMR analysis. Furthermore, GPC analysis demonstrated a significant shift towards lower mass fragments for the Cs2CO3-catalysed lignin degradation. A detailed GC-MS analysis for these samples identified a range of methoxy capped-monomeric degradation products. The scope of this reaction system was further expanded to lignocellulosic biomass such as milled beechwood chips, which notably showed similar product distributions. Based on the correlation of the experimental observations for extracted lignin samples and model compound studies, a mechanistic pathway for the Cs2CO3-catalysed system was suggested. DFT calculations provided reaction pathways for the observed cleavage products.
Design, synthesis, molecular docking, and in vitro antidiabetic activity of novel PPARγ agonist
Chaturvedi, Radha Nandan,Pendem, Krishnaiah,Patel, Vipul P.,Sharma, Mukta,Malhotra, Sunita
, p. 2069 - 2084 (2018/08/22)
Abstract: The present work describes the design, synthesis, molecular docking, biological evaluation, and assessment of structure–activity relationship of new derivatives based upon the molecular skeleton of the drug pioglitazone, a compound which is currently used for the management of type 2 diabetes mellitus. Pioglitazone has several side effects such as weight gain, edema, congestive heart failure, and bladder cancer. Therefore, there is a strong demand for identification of new lead candidates in the treatment of type 2 diabetes mellitus. A series of 24 compounds were prepared and evaluated for their peroxisome proliferator-activated receptor-γ (PPARγ) binding affinity assay and the IC50 values were determined. Among these compounds, six compounds exhibited promising IC50 values as compared to standard drugs pioglitazone and rosiglitazone. Furthermore, in order to confirm the target of these molecules, molecular docking study was carried out with peroxisome proliferator-activated receptor-γ (PPARγ) protein. Molecular modeling studies suggested that these compounds appropriately interact in the active sites of receptor. Graphical abstract: [Figure not available: see fulltext.].
ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANT
-
Paragraph 0026; 0149, (2013/03/28)
Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al.
