186191-19-5Relevant academic research and scientific papers
Rate accelerations of 1,3-dipolar cycloaddition reactions in ionic liquids
Fraga Dubreuil,Bazureau
, p. 7351 - 7355 (2000)
The 1,3-dipolar cycloaddition reactions between imidate 1 derived from diethyl aminomalonate and 2-ethoxybenzaldehyde 2 as dipolarophile has been investigated in various air and moisture stable ionic liquids. Significant rate enhancements and improved yie
Quantification and Prediction of Imine Formation Kinetics in Aqueous Solution by Microfluidic NMR Spectroscopy
Cao, Xiaoyu,Chen, Hang,Chen, Si,Ouyang, Jie,Tian, Zhongqun,Utz, Marcel,Wang, Xinchang,Wang, Xiuxiu,Yang, Liulin,You, Lei,Zhuo, Youzhen
, p. 9508 - 9513 (2021)
Quantitatively predicting the reactivity of dynamic covalent reaction is essential to understand and rationally design complex structures and reaction networks. Herein, the reactivity of aldehydes and amines in various rapid imine formation in aqueous sol
Inclusion of C60 into an adjustable porphyrin dimer generated by dynamic disulfide chemistry
Kieran, Amy L.,Pascu, Sofia I.,Jarrosson, Thibaut,Sanders, Jeremy K. M.
, p. 1276 - 1278 (2005)
A new, highly flexible porphyrin dimer was isolated in preparative scale from a dynamic disulfide library; this receptor adjusts to fit guests with a wide range of steric requirements and, whilst C60 proved to be an unsuitable template for this
New nitric oxide-releasing indomethacin derivatives with 1,3-thiazolidine-4-one scaffold: Design, synthesis, in silico and in vitro studies
Sava, Alexandru,Buron, Frederic,Routier, Sylvain,Panainte, Alina,Bibire, Nela,Profire, Lenu?a
, (2021/05/10)
In this study we present design and synthesis of nineteen new nitric oxide-releasing indomethacin derivatives with 1,3-thiazolidine-4-one scaffold (NO-IND-TZDs) (6a–s), as a new safer and efficient multi-targets strategy for inflammatory diseases. The che
Synthesis, antimicrobial evaluation, and in silico studies of quinoline—1H-1,2,3-triazole molecular hybrids
Awolade, Paul,Cele, Nosipho,Kerru, Nagaraju,Singh, Parvesh
, p. 2201 - 2218 (2020/06/17)
Abstract: Antimicrobial resistance has become a significant threat to global public health, thus precipitating an exigent need for new drugs with improved therapeutic efficacy. In this regard, molecular hybridization is deemed as a viable strategy to afford multi-target-based drug candidates. Herein, we report a library of quinoline—1H-1,2,3-triazole molecular hybrids synthesized via copper(I)-catalyzed azide-alkyne [3 + 2] dipolar cycloaddition reaction (CuAAC). Antimicrobial evaluation identified compound 16 as the most active hybrid in the library with a broad-spectrum antibacterial activity at an MIC80 value of 75.39?μM against methicillin-resistant S. aureus, E. coli, A. baumannii, and multidrug-resistant K. pneumoniae. The compound also showed interesting antifungal profile against C. albicans and C. neoformans at an MIC80 value of 37.69 and 2.36?μM, respectively, superior to fluconazole. In vitro toxicity profiling revealed non-hemolytic activity against human red blood cells (hRBC) but partial cytotoxicity to human embryonic kidney cells (HEK293). Additionally, in silico studies predicted excellent drug-like properties and the importance of triazole ring in stabilizing the complexation with target proteins. Overall, these results present compound 16 as a promising scaffold on which other molecules can be modeled to deliver new antimicrobial agents with improved potency. Graphic abstract: [Figure not available: see fulltext.].
Design, synthesis, in silico and in vitro studies for new nitric oxide‐releasing indomethacin derivatives with 1,3,4‐oxadiazole‐2‐thiol scaffold
Sava, Alexandru,Buron, Frederic,Routier, Sylvain,Panainte, Alina,Bibire, Nela,Constantin, Sandra M?d?lina,Lupa?cu, Florentina Geanina,Foc?a, Alin Viorel,Profire, Lenu?a
, (2021/07/07)
Starting from indomethacin (IND), one of the most prescribed non‐steroidal anti‐inflammatory drugs (NSAIDs), new nitric oxide‐releasing indomethacin derivatives with 1,3,4‐oxadiazole‐ 2‐thiol scaffold (NO‐IND‐OXDs, 8a‐p) have been developed as a safer and
5,6-dimethoxy indanone compound as well as preparation method and application thereof
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Paragraph 0022; 0043; 0048, (2019/10/17)
The invention discloses a 5,6-dimethoxy indanone compound as well as a preparation method and application thereof. The preparation method comprises the following steps: (1) by taking 3-hydroxybenzaldehyde as an initial raw material, in the presence of a f
Amine alkoxy chalcone compound and preparation method and application thereof
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Paragraph 0044; 0054, (2019/10/01)
The invention discloses an amine alkoxy chalcone compound, and a preparation method and application thereof. The preparation method comprises the following steps: (1) 3-hydroxybenzaldehyde is used as a starting material and reacts with a dibromide compoun
2'-Hydroxyl-3phenyl propiophenone compound and preparation method and application thereof
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Paragraph 0051; 0052, (2019/10/07)
The invention relates to a 2'-hydroxyl-3phenyl propiophenone compound and a preparation method and application thereof. The preparation method comprises the following steps that 1, 3-hydroxybenzaldehyde is used as an initial raw material, and under a firs
2-Benzoyl-6-benzylidenecyclohexanone analogs as potent dual inhibitors of acetylcholinesterase and butyrylcholinesterase
Leong, Sze Wei,Abas, Faridah,Lam, Kok Wai,Shaari, Khozirah,Lajis, Nordin H.
, p. 3742 - 3751 (2016/07/20)
In the present study, a series of 2-benzoyl-6-benzylidenecyclohexanone analogs have been synthesized and evaluated for their anti-cholinesterase activity. Among the forty-one analogs, four compounds (38, 39, 40 and 41) have been identified as lead compounds due to their highest inhibition on both AChE and BChE activities. Compounds 39 and 40 in particular exhibited highest inhibition on both AChE and BChE with IC50values of 1.6?μM and 0.6?μM, respectively. Further structure–activity relationship study suggested that presence of a long-chain heterocyclic in one of the rings played a critical role in the dual enzymes’ inhibition. The Lineweaver–Burk plots and docking results suggest that both compounds could simultaneously bind to the PAS and CAS regions of the enzyme. ADMET analysis further confirmed the therapeutic potential of both compounds based upon their high BBB-penetrating. Thus, 2-benzoyl-6-benzylidenecyclohexanone containing long-chain heterocyclic amine analogs represent a new class of cholinesterase inhibitor, which deserve further investigation for their development into therapeutic agents for cognitive diseases such as Alzheimer.
