- Ultrasound-assisted rapid and efficient one-pot synthesis of furanyl spirooxindolo and spiroquinoxalinopyrrolizidines by 1,3-dipolar cycloaddition: a green protocol
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Efficient synthesis of novel spirooxindolo and spiroquinoxalinopyrrolizidine derivatives was expediently accomplished with regioselectivity via one-pot, three-component 1,3-dipolar cycloaddition using ultrasonication. Chalcones derived from both heteroaryl methyl ketones and furfural were used as dipolarophiles in these reactions. The synthesized compounds were analyzed by 1H and 13C nuclear magnetic resonance (NMR), mass spectrometry, and elemental (CHN) analysis. Single-crystal X-ray diffraction studies of one of the compounds (11d) proved the structure and regiochemistry of the cycloaddition. The ultrasound methodology is clearly advantageous, and the desired products were obtained in moderate to good yield in shorter reaction time compared with conventional heating and fusion methods.
- Nishtala, Venkata Bharat,Nanubolu, Jagadeesh Babu,Basavoju, Srinivas
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- Synthesis of New Terpyridines under Solventless Conditions Using Alumina
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The preparation of terpyridine ligands under solventless conditions is presented. A new procedure using alumina as the base is described. This new procedure was applied to the preparation of new terpyridines.
- Husson, Jerome,Migianu, Evelyne,Beley, Marc,Kirsch, Gilbert
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- Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives
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For the development of new anticancer agents, 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2′:6′,2″-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were potent topoisomerase I inhibitors.
- Zhao, Long-Xuan,Kim, Tae Sung,Ahn, Soo-Hyun,Kim, Tae-Hyung,Kim, Eun-kyung,Cho, Won-Jea,Choi, Heesung,Lee, Chong-Soon,Kim, Jung-Ae,Jeong, Tae Cheon,Chang, Ching-jer,Lee, Eung-Seok
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- COMPOUNDS AND METHODS FOR TREATING OR PREVENTING HEART FAILURE
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The present invention relates to the discovery of novel compounds that can be used to treat and/or prevent heart failure in a subject. In certain embodiments, the compounds of the invention are sulfide: quinone oxidoreductase (SQOR) inhibitors. In other e
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Page/Page column 104; 129-130
(2020/07/25)
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- An Efficient Cyclic Di-AMP Based Artificial Metalloribozyme for Enantioselective Diels–Alder Reactions
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The diverse structures of nucleic acids as scaffolds have brought the significant advancement for DNA-based enantioselective catalysis, yet RNA-based enantioselective catalysis is lacking investigation. Herein, we report a small, natural RNA of cyclic di-AMP (c-di-AMP) and Cu2+ ions assemble into an artificial metalloribozyme (c-di-AMP·Cu2+), that could effectively catalyze the enantioselective Diels–Alder reactions with up to 80 percent ee. The enantioselective catalytic performance of c-di-AMP·Cu2+ has been studied by thorough investigations of different metal cofactors, c-di-AMP/Cu2+ molar ratios, additives, buffers and c-di-AMP analogues. In addition, the assembly of c-di-AMP·Cu2+ gives rise to 300-fold and 5-fold rate acceleration compared to the uncatalyzed reaction and Cu2+ ions, respectively. This work provides a simple and efficient strategy to construct the RNA-based catalysts that would expand the current nucleic acids-based catalysis and might hint the possible catalytic RNA in primordial chemistry.
- Qi, Qianqian,Lv, Shuting,Hao, Min,Dong, Xingchen,Gu, Youkun,Wu, Peizhe,Zhang, Wenyue,Chen, Yashao,Wang, Changhao
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p. 4417 - 4424
(2020/06/17)
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- Solvent-free enantioselective conjugate addition and bioactivities of nitromethane to Chalcone containing pyridine
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A series of chiral thioureas derived from quinine were tested as catalysts in the enantioselective Michael additions of nitromethane to α,β-unsaturated ketones containing pyridine. The best results were obtained with the bifunctional catalyst prepared from 3,5-di(trifluoromethyl)-aniline under solvent-free conditions. This thiourea promoted the reaction with high enantioselectivities and chemical yields for aryl ketones. The origins of enantioselectivity were further investigated via experiment and computation. Meanwhile, the products from our reaction showed potent antibacterial activities against rice bacterial leaf blight, with the S-enantiomer performing much better than the R-enantiomer. Given the promising bioactivity of this class of molecules, our work is expected to offer important applications in developing future generations for drug design.
- Zhang, Guoping,Zhu, Chun,Liu, Dengyue,Pan, Jianke,Zhang, Jian,Hu, Deyu,Song, Baoan
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p. 129 - 136
(2016/12/23)
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- N-Heterocyclic carbene-catalyzed diastereoselective synthesis of β-lactone-fused cyclopentanes using homoenolate annulation reaction
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NHC-catalyzed annulation of enals with 2-enoylpyridines or 2-enoylpyridine N-oxides leading to the diastereoselective synthesis of β-lactone-fused cyclopentanes is reported. The reaction proceeds via the generation of homoenolate equivalent intermediates and tolerates a broad range of functional groups.
- Mukherjee, Subrata,Mondal, Santigopal,Patra, Atanu,Gonnade, Rajesh G.,Biju, Akkattu T.
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supporting information
p. 9559 - 9562
(2015/06/08)
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- Diastereo- and enantioselective direct vinylogous Michael addition of γ-substituted butenolides to 2-enoylpyridines catalyzed by chiral bifunctional amine-squaramides
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The diastereo- and enantioselective direct vinylogous Michael addition reaction of γ-substituted butenolides to 2-enoylpyridines has been achieved. A range of γ,γ-disubstituted butenolide derivatives, bearing two consecutive tri- and tetrasubstituted stereogenic centers, were readily obtained in good yields with excellent stereoselectivities (up to >99:1 dr and >99% ee).
- Wang, Zhen-Hua,Wu, Zhi-Jun,Huang, Xue-Qun,Yue, Deng-Feng,You, Yong,Xu, Xiao-Ying,Zhang, Xiao-Mei,Yuan, Wei-Cheng
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supporting information
p. 15835 - 15838
(2015/11/10)
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- Photophysical properties of new cyclometalated ruthenium complexes and their use in dye sensitized solar cells
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A new class of cyclometalated ruthenium complexes, Ru(C^N^N′) (N^N′^N′′)·Cl where N^N′^N′′ = 4,4′,4′′-tricarboxy-2,2′:6′,2′′- terpyridine and C^N^N′ = substituted 6-phenyl-2,2′-bipyridine, for Dye Sensitized Solar Cells (DSSCs) is proposed. We have investigated the effect of different substituents (R = COOH, thiophen-2-yl, F and OCH3) on the ancillary C^N^N′ ligand on the photophysical properties and performance of the six different cyclometalated ruthenium complexes in DSSCs. Using an ionic liquid based electrolyte, efficiencies up to η = 3.06% have been attained under 1 sun irradiation. Moreover, the T66 based DSSC exhibited a good stability under 1000 W m2 light soaking at 60 °C for 24 days, retaining 92.8% of its initial efficiency.
- Kisserwan, Hawraa,Kamar, Amanda,Shoker, Tharallah,Ghaddar, Tarek H.
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p. 10643 - 10651
(2013/01/14)
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- NOVEL PROPENONE DERIVATIVES CONTAINING AROMATIC RINGS, A MAUFACTURING PROCESS THEREOF AND A COMPOSITION CONTAINING THE SAME USING AS AN ANTIINFLAMMATORY AGENT
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The present invention is related to novel propenone derivatives containing aromatic ring, a manufacturing process thereof and a composition containing the same using as an anti? inflammatory agent. The compound of the present invention show potent anti-inflammatory activity confirmed by various experiments for example, the inhibition test of COX and 5-LOX enzyme activity, the inhibition test of LTC reproduction and NO production, MTT assay test, the inhibition test on the iNOS and COX-2 protein expression and PGE reproduction using RAW 264.7 macrophage etc. Accordingly, present compounds can be useful in treating and preventing various inflammatory.
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Page/Page column 11-12
(2010/02/15)
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- Simple aromatic compounds containing propenone moiety show considerable dual COX/5-LOX inhibitory activities
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For the development of safer anti-inflammatory agents, simple aromatic compounds containing propenone moiety were prepared and evaluated for their dual COX/5-LOX inhibitory activities. Among the 17 prepared compounds, most of the compounds exhibited considerable COX/5-LOX inhibitory activities. Especially compound C15 showed the most significant dual COX/5-LOX inhibitory activity.
- Jahng, Yurngdong,Zhao, Long-Xuan,Moon, Yoon-Soo,Basnet, Arjun,Kim, Eun-Kyung,Chang, Hyeun Wook,Ju, Hye Kyung,Jeong, Tae Cheon,Lee, Eung-Seok
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p. 2559 - 2562
(2007/10/03)
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- Synthesis and Characterization of Fluorescent 4,6-Disubstituted-3-cyano-2-methylpyridines
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4,6-Disubstituted-3-cyano-2-methylpyridines, easily prepared by treating α,b-unsaturated carbonyl compounds with β-aminocrotononitrile in the presence of potassium tert-butoxide, have been found to show intense fluorescence in the region of 400-552 nm. 3-
- Matsui, Masaki,Oji, Akira,Hiramatsu, Koichi,Shibata, Katsuyoshi,Muramatsu, Hiroshige
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p. 201 - 206
(2007/10/02)
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- Synthesis of 3-Cyano-2-methylpyridines Substituted with Heteroaromatics
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A series of title compounds were easily prepared by the sonication of α,β-unsaturated carbonyl compound in acetonitril in the presence of potassium t-butoxide.
- Shibata, Katsuyoshi,Katsuyama, Isamu,Matsui, Masaki,Muramatsu, Hiroshiga
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p. 161 - 165
(2007/10/02)
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