- Reactions of cyclic enhydrazinoketones with arylidene derivatives of malononitrile. Synthesis of fused N-substituted 1,4-dihydropyridines
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A new method for the synthesis of fused N-amino-1,4-dihydropyridines was proposed. The method is based on the addition of cyclic enhydrazinoketones to arylidenemalononitriles. The structures of the compounds synthesized were studied using 1H NMR spectroscopy.
- Lichitsky,Yarovenko,Zavarzin,Krayushkin
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- Discovery of tetrahydrocarbazoles as dual pERK and pRb inhibitors
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The extracellular signal-regulated kinase (ERK) is one of the most important molecular targets for cancer that controls diverse cellular processes such as proliferation, survival, differentiation and motility. Similarly, the Rb (retinoblastoma protein) is
- Kulkarni, Mahesh R.,Mane, Madhav S.,Ghosh, Usha,Sharma, Rajiv,Lad, Nitin P.,Srivastava, Ankita,Kulkarni-Almeida, Asha,Kharkar, Prashant S.,Khedkar, Vijay M.,Pandit, Shivaji S.
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p. 366 - 378
(2017/04/24)
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- Library design, synthesis and biological exploration of novel 3,4′-bicarbostyril derivatives as potent antimicrobial, antitubercular and antimalarial agents
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Abstract: A library comprises diversely substituted novel 3,4′-bicarbostyril derivatives have been designed by molecular hybridization technique and synthesized via multi-component reaction. Compounds G22 (MIC = 12.5 μg/mL) and G38 (MIC = 25 μg/mL) exhibited 99% inhibition against Mycobacterium tuberculosis, while compounds G40 (IC50 = 0.019 μg/mL) and G20 (IC50 = 0.028 μg/mL) found to have excellent activity against Plasmodium falciparum. Compounds G37 (MIC = 25 μg/mL) and G8, G18, and G38 (MIC = 50 μg/mL) elicited excellent antimicrobial activity compared to standard drugs. Biological results revealed that the potency of the title compounds strongly depends on the length and flexibility of various spacers at N?1, the electronic influence of substituent at R1 and lipophilicity of CH3 group at R2 position on bicarbostyril system. Graphical Abstract: [InlineMediaObject not available: see fulltext.]
- Jardosh, Hardik H.,Vala, Nileshkumar D.,Patel, Manish P.
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p. 881 - 899
(2017/04/13)
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- Microwave-irradiated synthesis of 1,2-dihydropyridines from n-functionalized enaminones and enals through domino condensation and 6π-azaelectrocyclization
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N-Amino-substituted 1,2-dihydropyridine motifs are constructed using cyclohexane-1,3-diones via the Knoevenagel condensation with enals followed by 6π-electrocyclization using ethylenediammonium diacetate as a catalyst under MW irradiation. A survey of su
- Shaban, Elkhabiry,Hossain, Md. Imran,Wu, Ming-Yu,Takemasa, Yoshihiko,Nagae, Sachie,Peng, Wei,Kawafuchi, Hiroyuki,Inokuchi, Tsutomu
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p. 171 - 182
(2014/02/14)
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- Synthesis of [1,2]oxazolo[5,4-e]indazoles as antitumour agents
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A series of 40 derivatives of the [1,2]oxazolo[5,4-e]indazoles ring system have been prepared with good yields using a versatile and convenient route. Annelation of the [1,2]oxazole ring on the indazole-4-one system was achieved by reaction of the corresp
- Barraja, Paola,Spanò, Virginia,Giallombardo, Daniele,Diana, Patrizia,Montalbano, Alessandra,Carbone, Anna,Parrino, Barbara,Cirrincione, Girolamo
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supporting information
p. 6474 - 6477
(2013/07/26)
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- 3-Aryl- and 2,3-diaryl-4-oxo-4,5,6,7-tetrahydro-indazoles. 1. Reactions of phenyl- and tosyl-hydrazones of dimedone and cyclohexane-1,3-dione with substituted benzaldehydes
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Sixteen 3-aryl-4-oxo-2-phenyl-4,5,6,7-tetrahydroindazoles were obtained from the reaction of the phenylhydrazones of dimedone and cyclohexane-1,3-dione with 3-bromo-, 4-bromo-, 4-chloro-, 4-fluoro-, 2-hydroxy-, 4-hydroxy-, 4-methoxy-, 2-nitro-, 3-nitro-,
- Strakova,Strakovs,Petrova
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p. 1398 - 1404
(2007/10/03)
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- 4-hydroxy derivatives of 5,6,9,10-tetrahydro-10-((2-methyl-1h-imidazol-1-yl)methyl)-4h-pyrido-(3,2,1-jk)-carbazol-11(8h)-one
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The present invention relates to novel 4-hydroxy derivatives of 5,6,9,10-tetrahydro-10-[(2-methyl-1H-imidazol-1-yl)methyl]-4H-pyrido-[3,2,1-jk]-carbazol-11(8H)-one with 5-HT3-receptor antagonistic activity. Furthermore, the invention relates to a process for the preparation of the novel derivatives.
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