- Microwave-assisted organic acid-base-co-catalyzed tandem Meinwald rearrangement and annulation of styrylepoxides
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A novel organic acid-base-co-catalyzed conversion of styrylepoxides into [1,1′-biaryl]-3-carbaldehydes was realized under microwave irradiation. Styrylepoxides first underwent an acid-catalyzed Meinwald rearrangement followed by a tandem base-catalyzed Michael addition, aldol addition, and aromatization sequence to generate [1,1′-biaryl]-3-carbaldehydes.
- Shi, Yi,Li, Siqi,Lu, Yang,Zhao, Zizhen,Li, Pingfan,Xu, Jiaxi
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supporting information
p. 2131 - 2134
(2020/02/27)
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- Phenylpropiolic acid small molecular organic compounds and synthetic method and application thereof
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The invention relate to a category of novel phenylpropiolic acid small molecular organic compounds as shown in a structural formula (I) or stereisomers, crystals, hydrates or pharmaceutically acceptable salt and an application of the phenylpropiolic acid small molecular organic compounds or stereisomers, crystals, hydrates or pharmaceutically acceptable salt and pharmaceutical compositions comprising the compounds in preparing a GPR40 agonist and drugs for promoting insulin release, treating and/or preventing diabetes or complications, treating diabetes inducing poor therapeutic effect inducedby acquired drug-resistance and complications and the like. The invention also provides a preparation method of the phenylpropiolic acid small molecular organic compounds as shown in the structural formula (I). The phenylpropiolic acid small molecular organic compounds have good anti-diabetes effect and the risk of inducing hypoglycemia is lower than that of conventional drugs.
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Paragraph 0074; 0075; 0104; 0105; 0106
(2019/04/13)
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- 4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors
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This study reports on a preliminary structure-activity relationship exploration of 4-aryliden-2-methyloxazol-5(4H)-one-based compounds as MAGL/FAAH inhibitors. Our results highlight that this scaffold may serve for the development of selective MAGL inhibi
- Granchi, Carlotta,Rizzolio, Flavio,Bordoni, Vittorio,Caligiuri, Isabella,Manera, Clementina,Macchia, Marco,Minutolo, Filippo,Martinelli, Adriano,Giordano, Antonio,Tuccinardi, Tiziano
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p. 137 - 146
(2016/01/12)
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- Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites
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The potential of azaaurones as dual-stage antimalarial agents was investigated by assessing the effect of a small library of azaaurones on the inhibition of liver and intraerythrocytic lifecycle stages of the malaria parasite. The whole series was screened against the blood stage of a chloroquine-resistant Plasmodium falciparum strain and the liver stage of P. berghei, yielding compounds with dual-stage activity and sub-micromolar potency against erythrocytic parasites. Studies with genetically modified parasites, using a phenotypic assay based on the P. falciparum Dd2-ScDHODH line, which expresses yeast dihydroorotate dehydrogenase (DHODH), showed that one of the azaaurone derivatives has the potential to inhibit the parasite mitochondrial electron-transport chain. The global urgency in finding new therapies for malaria, especially against the underexplored liver stage, associated with chemical tractability of azaaurones, warrants further development of this chemotype. Overall, these results emphasize the azaaurone chemotype as a promising scaffold for dual-stage antimalarials.
- Carrasco, Marta P.,Machado, Marta,Gon?alves, Lídia,Sharma, Moni,Gut, Jiri,Lukens, Amanda K.,Wirth, Dyann F.,André, Vania,Duarte, Maria Teresa,Guedes, Rita C.,dos Santos, Daniel J. V. A.,Rosenthal, Philip J.,Mazitschek, Ralph,Prudêncio, Miguel,Moreira, Rui
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supporting information
p. 2194 - 2204
(2016/10/19)
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS FOR THE TREATMENT OF DISEASES
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Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
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Paragraph 000943
(2015/04/15)
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- Inhibition of prostaglandin E2 production by synthetic minor prenylated chalcones and flavonoids: Synthesis, biological activity, crystal structure, and in silico evaluation
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The discovery of potent inhibitors of prostaglandin E2 (PGE 2) synthesis in recent years has been proven to be an important game changer in pharmaceutical industry. It is known that excessive production of PGE2 triggers a
- Rullah, Kamal,Mohd Aluwi, Mohd Fadhlizil Fasihi,Yamin, Bohari M.,Abdul Bahari, Mohd Nazri,Wei, Leong Sze,Ahmad, Syahida,Abas, Faridah,Ismail, Nor Hadiani,Jantan, Ibrahim,Wai, Lam Kok
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p. 3826 - 3834
(2014/09/16)
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- Palladium-catalyzed Suzuki-Miyaura coupling of aryl sulfamates with arylboronic acids
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Readily available NHC-Pd(ii)-Mp complexes 2 showed efficient catalytic activity toward the Suzuki-Miyaura coupling of aryl sulfamates with arylboronic acids or potassium phenyltrifluoroborate, giving the expected coupling products in good to high yields.
- Wang, Zhan-Yong,Ma, Qin-Na,Li, Ren-Hao,Shao, Li-Xiong
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p. 7899 - 7906
(2013/11/19)
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- Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNFα-induced nuclear factor-κB activation inhibition
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A series of biaryl-based chalcones were designed as a combination of the natural chalcone and biphenyl moieties, and synthesized by two step chemistry involving Knoevenagel reaction and microwave assistant Suzuki coupling. Sulforhodamine B (SRB) assay was performed to evaluate the cell viability inhibitory abilities of these compounds against five cancer cell lines (A549, CNE2, SW480, MCF-7, and HepG2) from different tissues. Their Nuclear Factor-κB (NF-κB) nuclear translocation inhibitory activities were further investigated by High Content Analysis (HCA) based assay. Most of the compounds showed moderate to strong anticancer and NF-κB nuclear translocation inhibition activities and potent compounds were found.
- Zuo, Yinglin,Yu, Yi,Wang, Shuni,Shao, Weiyan,Zhou, Binhua,Lin, Li,Luo, Zhuoyu,Huang, Ruogu,Du, Jun,Bu, Xianzhang
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experimental part
p. 393 - 404
(2012/07/27)
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