20118-38-1Relevant academic research and scientific papers
Chemoselective reduction of ?,¢-unsaturated carbonyl and carboxylic compounds by hydrogen iodide
Matsumoto, Shoji,Marumoto, Hayato,Akazome, Motohiro,Otani, Yasuhiko,Kaiho, Tatsuo
, p. 590 - 599 (2021/03/29)
The selective reduction of ?,¢-unsaturated carbonyl compounds was achieved to produce saturated carbonyl compounds with aqueous HI solution. The introduction of an aryl group at an ? or ¢ position efficiently facilitated the reduction with good yield. The reaction was applicable to compounds bearing carboxylic acids and halogen atoms. Through the investigation of the reaction mechanism, it was found that Michael-type addition of iodide occurred to produce ¢-iodo compounds followed by the reduction of C-I bond via anionic and radical paths.
Fluorescent Molecular Logic Gates Driven by Temperature and by Protons in Solution and on Solid
West, Matthew E. S.,Yao, Chao-Yi,Melaugh, Gavin,Kawamoto, Kyoko,Uchiyama, Seiichi,de Silva, A. Prasanna
supporting information, p. 13268 - 13274 (2021/08/06)
Temperature-driven fluorescent NOT logic is demonstrated by exploiting predissociation in a 1,3,5-trisubstituted Δ2-pyrazoline on its own and when grafted onto silica microparticles. Related Δ2-pyrazolines become proton-driven YES an
Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis
Sahoo, Santosh Kumar,Rani, Bandela,Gaikwad, Nikhil Baliram,Ahmad, Mohammad Naiyaz,Kaul, Grace,Shukla, Manjulika,Nanduri, Srinivas,Dasgupta, Arunava,Chopra, Sidharth,Yaddanapudi, Venkata Madhavi
, (2021/06/14)
In search of novel therapeutic agents active against emerging drug-resistant Mycobacterium tuberculosis and to counter the long treatment protocol of existing drugs, herein we present synthesis and biological evaluation of a new series of 5-phenyl-3-isoxazolecarboxylic acid methyl ester-chalcone hybrids. Among 35 synthesized compounds, 32 analogues displayed potent in-vitro activity against Mycobacterium tuberculosis H37Rv with MIC 0.12–16 μg/mL. Cell viability test against Vero cells indicated 29 compounds to be non-cytotoxic (CC50 > 20 μg/mL & SI > 10). Most potent compounds with MIC 0.12 μg/mL (7 b, 7j, 7 ab) exhibited selectivity index (SI) in excess of 320. Further studies on activity against drug-resistant Mycobacterium tuberculosis revealed 7j as the most potent compound with MIC 0.03–0.5 μg/mL. Time-kill kinetic study suggested compound 7j displaying concentration-dependent bactericidal killing activity with relatively comparable potency to that of current first-line anti-TB drugs. Taken together, 7j presents a novel hit with potential to be translated into a potent antimycobacterial.
Microwave-assisted Synthesis and Molecular Docking Study of Heteroaromatic Chalcone Derivatives as Potential Antibacterial Agents
Farooq, Saba,Mortadza, Nur Arif,Ngaini, Zainab
supporting information, (2020/09/09)
In this study, a series of chalcone derivatives (1a–c) were synthesized via Claisen-Schmidt condensation, followed by aza-Michael addition to form pyrazoline derivatives (2a–c and 3a–c). The reaction was performed via microwave radiation to give excellent
A chalcone derivative binds a putative allosteric site of YopH: Inhibition of a virulence factor of Yersinia
Botta, Maurizio,Domeneghini Chiaradia-Delatorre, Louise,Menegatti, Angela C. O.,Mori, Mattia,Nunes, Ricardo J.,Rocha, Ruth F.,Sens, Larissa,Terenzi, Hernán,Tizziani, Tiago,de Souza, Ana C. A.,de Souza, Luiz F. S.
supporting information, (2020/06/25)
Identification of allosteric inhibitors of PTPs has attracted great interest as a new strategy to overcome the challenge of discover potent and selective molecules for therapeutic intervention. YopH is a virulence factor of the genus Yersinia, validated a
CYCLOADDITION REACTIONS USING QUANTUM DOTS
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Paragraph 0131-0132, (2020/11/30)
Disclosed herein are methods in which colloidal quantum dots (QDs) can serve as visible-light chromophores, photocatalysts, and reusable scaffolds for homo- and hetero-intermolecular [2+2] photocycloadditions. The methods may lead to >90% tunable regiosel
Synthesis of Kojic Ester Derivatives as Potential Antibacterial Agent
Sie, Carolynne Zie Wei,Ngaini, Zainab,Suhaili, Nurashikin,Madiahlagan, Eswaran
, (2018/06/04)
The search for lead product with beneficial pharmacological properties has become a great challenge and costly. Extraction and synthetic modification of bioactive compounds from natural resources has gained great attention and is cost effective. In this study, kojic acid was produced from fungal fermentation, using sago waste as substrate, and chemically incorporated with chalcones and azobenzene to form a series of kojic ester derivatives and evaluated for antibacterial activities. Kojic ester bearing halogenated chalcone demonstrated active inhibition against Staphylococcus aureus compared to that of standard ampicillin. The inhibition increased as the electronegativity of halogens decreased, while incorporation of azobenzene derivatives on kojic acid backbone demonstrated fair antibacterial activity against Escherichia coli with minimum inhibitory concentration (MIC) of 190-330 ppm. The presence of C=C and N=N reactive moieties in both chalcone and azo molecules contributed to the potential biological activities of the kojic acid ester.
Novel 1,3,4-thiadiazole-chalcone hybrids containing catechol moiety: synthesis, antioxidant activity, cytotoxicity and DNA interaction studies
Jakovljevi?, Katarina,Joksovi?, Milan D.,Mati?, Ivana Z.,Petrovi?, Nina,Stanojkovi?, Tatjana,Sladi?, Du?an,Vuj?i?, Miroslava,Janovi?, Barbara,Joksovi?, Ljubinka,Trifunovi?, Sne?ana,Markovi?, Violeta
, p. 1679 - 1697 (2018/10/26)
Hybrid compounds that combine the 1,3,4-thiadiazole-containing catechol moiety with a chalcone motif were synthesized and examined for their antioxidant activity, cytotoxicity, and DNA-binding activity. A series of thirteen compounds showed strong antioxi
Activation of anti-oxidant Nrf2 signaling by enone analogues of curcumin
Deck, Lorraine M.,Hunsaker, Lucy A.,Vander Jagt, Thomas A.,Whalen, Lisa J.,Royer, Robert E.,Vander Jagt, David L.
supporting information, p. 854 - 865 (2017/12/13)
Inflammation and oxidative stress are common in many chronic diseases. Targeting signaling pathways that contribute to these conditions may have therapeutic potential. The transcription factor Nrf2 is a major regulator of phase II detoxification and anti-oxidant genes as well as anti-inflammatory and neuroprotective genes. Nrf2 is widespread in the CNS and is recognized as an important regulator of brain inflammation. The natural product curcumin exhibits numerous biological activities including ability to induce the expression of Nrf2-dependent phase II and anti-oxidant enzymes. Curcumin has been examined in a number of clinical studies with limited success, mainly owing to limited bioavailability and rapid metabolism. Enone analogues of curcumin were examined with an Nrf2 reporter assay to identify Nrf2 activators. Analogues were separated into groups with a 7-carbon dienone spacer, as found in curcumin; a 5-carbon enone spacer with and without a ring; and a 3-carbon enone spacer. Activators of Nrf2 were found in all three groups, many of which were more active than curcumin. Dose-response studies demonstrated that a range of substituents on the aromatic rings of these enones influenced not only the sensitivity to activation, reflected in EC50 values, but also the extent of activation, which suggests that multiple mechanisms are involved in the activation of Nrf2 by these analogues.
Including yinyin zuo of chalcone derivatives and use thereof
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Paragraph 0048; 0049, (2018/10/19)
The invention including yinyin zuo of chalcone derivatives and its application. As shown in general formula I including yinyin zuo of chalcone derivatives and their pharmaceutically acceptable salt, hydrate, solvate or prodrug has anti-tumor effect. The i
