- Synthesis, biological evaluation and structure-activity relationships of 5-arylidene tetramic acids with antibacterial activity against methicillin-resistant Staphylococcus aureus
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The steady rise of the antimicrobial resistance is a major global threat to human health that requires the urgent need for novel antibiotics. In this work we report the synthesis of a small library of 3-subsituted-5-arylidene tetramic acids in order to in
- Matiadis, Dimitris,Tsironis, Dimitrios,Stefanou, Valentina,Boussias, Spyridon,Panagiotopoulou, Angeliki,McKee, Vickie,Igglessi-Markopoulou, Olga,Markopoulos, John
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Read Online
- An Atropos Chiral Biphenyl Bisphosphine Ligand Bearing Only 2,2′-Substituents and Its Application in Rh-Catalyzed Asymmetric Hydrogenation
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An atropos chiral biphenyl bisphosphine ligand bearing only 2,2′-substituents was rationally designed and easily synthesized utilizing a bulky chiral t-butylmethylphosphino block. Computational results showed a large difference in the free energies betwee
- Jia, Jia,Ling, Zheng,Zhang, Zhenfeng,Tamura, Ken,Gridnev, Ilya D.,Imamoto, Tsuneo,Zhang, Wanbin
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supporting information
p. 738 - 743
(2017/12/26)
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- Green fluorescent protein chromophore derivatives as a new class of aldose reductase inhibitors
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A number of (Z)-4-arylmethylene-1H-imidazol-5(4H)-ones, which are related to the fluorescent chromophore of the Aequorea green fluorescent protein (GFP), have been synthesized and evaluated their in vitro inhibitory activity against recombinant human aldo
- Saito, Ryota,Hoshi, Maiko,Kato, Akihiro,Ishikawa, Chikako,Komatsu, Toshiya
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p. 965 - 974
(2016/10/25)
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- Synthesis of Indole-2-carboxylate Derivatives via Palladium-Catalyzed Aerobic Amination of Aryl C-H Bonds
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A direct oxidative C-H amination affording 1-acetyl indolecarboxylates starting from 2-acetamido-3-arylacrylates has been achieved. Indole-2-carboxylates can be targeted with a straightforward deacetylation of the initial reaction products. The C-H amination reaction is carried out using a catalytic Pd(II) source with oxygen as the terminal oxidant. The scope and application of this chemistry is demonstrated with good to high yields for numerous electron-rich and electron-poor substrates. Further reaction of selected products via Suzuki arylation and deacetylation provides access to highly functionalized indole structures.
- Clagg, Kyle,Hou, Haiyun,Weinstein, Adam B.,Russell, David,Stahl, Shannon S.,Koenig, Stefan G.
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supporting information
p. 3586 - 3589
(2016/08/16)
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- SERINE/THREONINE KINASE INHIBITORS
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Compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such diseases, or associated pathological conditions are disclosed.
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Paragraph 00388
(2015/07/16)
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- An efficient and green synthesis of benzylidene-2-N-(carbothioamido)-6-oxo-1,2,5,6-tetrahydro-1-NH-1,2,4-triazine derivatives and their antibacterial activity evaluation
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An efficient and green synthesis of (Z)-3-allkyl-5(benzylidene/substituted benzylidene)-2N-(carbothioamido)-6-oxo-1,2,5,6-tetrahydro-1-NH-1,2,4-triazine derivatives have been developed in good yields and tested for their antibacterial activities against Escherichia coli, Providencia aeruginosa, Pseudomonas azotogensis and Baccilus subtillis. Some of the synthesized compounds possess good activity against Escherichia coli and Baccilus subtillis compared to standard drug streptomycin.
- Rani, V. Anitha,Kumari, Y. Bharathi
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p. 5931 - 5934
(2015/02/19)
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- Synthesis of novel cinnamanilides as potential immunosuppressive agents
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A series of new cinnamanilides (6-40) were synthesized and their immunosuppressive activity and cytotoxicity were evaluated. Most of the cinnamanilides showed good immunosuppressive activity. Among the synthesized compounds, (Z)-N-(4-bromophenyl)-2-methox
- Shi, Lei,Wang, Lu,Wang, Zhi,Zhu, Hai-Liang,Song, Qiao
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experimental part
p. 585 - 593
(2012/02/14)
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- Pseudo-peptides derived from isomannide: Inhibitors of serine proteases
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In this paper, we describe the synthesis of a novel class of pseudo-peptides derived from isomannide and several oxazolones as potential inhibitors of serine proteases as well as preliminary pharmacological assays for hepatitis C. Hepatitis C, dengue and West Nile fever are among the most important flaviviruses that share one important serine protease enzyme. Serine proteases belong to the most studied class of proteolytic enzymes and are a primary target in the drug development field. Several pseudo-peptides were obtained in good yields from the reaction of isomannide and oxazolones, and their anti-HCV potential using the HCV replicon-based assay was shown.
- Barros, Thalita G.,Pinheiro, Sergio,Williamson,Tanuri, Amilcar,Gomes Jr.,Pereira, Helena S.,Brindeiro,Neto, Jose B. A.,Antunes,Muri, Estela M. F.
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scheme or table
p. 701 - 709
(2010/08/05)
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- Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones
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A series of thirteen 4,5-diaryl-3-hydroxy-2(5H)-furanones were synthesized. They were evaluated for their antioxidant potencies and inhibitory properties of 5-lipoxygenase, cyclooxygenases, HIV-1 integrase and PC3 cell proliferation. New hits were discove
- Bailly, Fabrice,Queffelec, Clemence,Mbemba, Gladys,Mouscadet, Jean-Francois,Pommery, Nicole,Pommery, Jean,Henichart, Jean-Pierre,Cotelle, Philippe
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p. 1222 - 1229
(2008/09/20)
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- Synthesis of (S)-3,4-dihydroxyphenylalanine (L-DOPA) and unnatural α-amino acids via enzymatic resolution using alcalase
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Enzymatic resolution has been used for the synthesis of L-DOPA with high optical purity.N-Acetyl-(R,S)-3,4-methylenedioxyphenylalanine methyl ester (2b) on enzymatic resolution by alcalase (Subtilisin Carlsberg) yields N-acetyl-(S)-3,4-methylenedioxyphenylalanine (3b) which upon acid treatment affords (S)-3,4-dihydroxyphenylalanine (L-DOPA) (4).Several optically active unnatural N-acetylated and N-benzoylated α-amino acids have been prepared by similar enzymatic resolution.
- Tyagi, O D,Boll, P M,Parmar, V S,Taneja, Poonam,Singh, S K
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p. 851 - 854
(2007/10/02)
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