- Synthesis and evaluation of anti-Tuberculosis and anti-cancer activities of hydrazones and N-Acylhydrazones by using sonochemistry, a new general procedure
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Background: In continuation of our research on sonochemistry and due to the importance and application of hydrazones and N-Acylhydrazones in drug discovery, in this work we report a new general and efficient synthesis of these classes with different aromatic and heteroaromatic nucleus assisted by ultrasound and their respective anti-Tuberculosis and anti-cancer activities. Method: Derivatives 7-chloroquinoline 10 and 12 were the most promising compounds against cancer and TB, respectively. Conclusion: Unfortunately all new hydrazones and N-Acylhydrazones evaluated displayed no activity anti cancer and TB.
- Da Silveira Pinto, Ligia S.,De Souza, Marcus V. N.,Kaiser, Carlos R.
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p. 678 - 685
(2017/07/15)
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- Structure-Based Rational Design of Novel Inhibitors Against Fructose-1,6-Bisphosphate Aldolase from Candida albicans
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Class II fructose-1,6-bisphosphate aldolases (FBA-II) are attractive new targets for the discovery of drugs to combat invasive fungal infection, because they are absent in animals and higher plants. Although several FBA-II inhibitors have been reported, none of these inhibitors exhibit antifungal effect so far. In this study, several novel inhibitors of FBA-II from C. albicans (Ca-FBA-II) with potent antifungal effects were rationally designed by jointly using a specific protocols of molecular docking-based virtual screening, accurate binding-conformation evaluation strategy, synthesis and enzymatic assays. The enzymatic assays reveal that the compounds 3c, 3e-g, 3j and 3k exhibit high inhibitory activity against Ca-FBA-II (IC50 50 value of 2.7 μM. Importantly, the compounds 3f, 3g, and 3l possess not only high inhibitions against Ca-FBA-II, but also moderate antifungal activities against C. glabrata (MIC80 = 4-64 μg/mL). The compounds 3g, 3l, and 3k in combination with fluconazole (8 μg/mL) displayed significantly synergistic antifungal activities (MIC80 0.0625 μg/mL) against resistant Candida strains, which are resistant to azoles drugs. The probable binding modes between 3g and the active site of Ca-FBA-II have been proposed by using the DOX (docking, ONIOM, and XO) strategy. To our knowledge, no FBA-II inhibitors with antifungal activities against wild type and resistant strains from Candida were reported previously. The positive results suggest that the strategy adopted in this study are a promising method for the discovery of novel drugs against azole-resistant fungal pathogens in the future.
- Han, Xinya,Zhu, Xiuyun,Hong, Zongqin,Wei, Lin,Ren, Yanliang,Wan, Fen,Zhu, Shuaihua,Peng, Hao,Guo, Li,Rao, Li,Feng, Lingling,Wan, Jian
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p. 1426 - 1438
(2017/07/03)
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- TETRAZOLIUM COMPOUND FOR DETECTING MICROORGANISMS, REAGENT FOR DETECTING MICROORGANISMS AND METHOD FOR DETECTING MICROORGANISMS
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The object of the present invention is to provide a compound used in a reagent for detecting microorganisms, by which microorganisms can be rapidly and reliably detected without requiring any special instrument, the reagent for detecting microorganisms, a
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Paragraph 0035; 0036
(2013/03/26)
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- Functional group transformations in derivatives of 6-oxoverdazyl
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Transformations of functional groups, such as OCH2Ph, OCOPh, NO2 and I, in 1,3,5-triphenyl-6-oxoverdazyls 1a-1e were investigated in order to expand the range of synthetic tools for incorporation of the verdazyl system into more complex molecular architectures and to increase spin delocalization. Thus, Pd-catalyzed debenzylation of the OCH2Ph group or basic hydrolysis of the OCOPh group gave the phenol functionality, which was acylated, but could not be alkylated. Orthogonal deprotection of diphenol functionality was also demonstrated in radical 1c. Pt-catalyzed reduction of the NO2 group led to the aniline derivative, which was acylated. Attempted C-C coupling reactions to iodophenyl derivatives 1e and 5e were unsuccessful. Selected verdazyl radicals were characterized by EPR and electronic absorption spectroscopy, and results were analyzed with the aid of DFT computational methods.
- Jasinski, Marcin,Gerding, Jason S.,Jankowiak, Aleksandra,Geibicki, Krzysztof,Romanski, Jaroslaw,Jastrzeibska, Katarzyna,Sivaramamoorthy, Ajan,Mason, Kristein,Evans, Donavan H.,Celeda, Malgorzata,Kaszynski, Piotr
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p. 7445 - 7454
(2013/09/02)
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- Ultrasound assisted syntheses of some 1,2,4-triazole derivatives
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A facile preparation of a series of 1,2,4-triazole derivatives under ultrasound irradiation, that proceeded via one-pot reaction of a- nitrophenyl hydrazones with different methylene amines, using sodium nitrite as oxidant and benzyl triethyl ammonium chloride (BTEAC) as phase transfer catalysis, respectively, was described.
- Wang, Yingchun,Yi, Xianghui,Qin, Wen
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experimental part
p. 217 - 219
(2012/08/07)
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- Synthesis and properties of pyrazolino[60]fullerene-donor systems
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A series of pyrazolino[60]fullerenes has been prepared in one pot by 1,3-dipolar cycloaddition to C60 of the corresponding nitrile imine, which was generated in situ from the corresponding hydrazone. A range of donors and acceptors were introdu
- Espíldora, Eva,Delgado, Juan Luis,De La Cruz, Pilar,De La Hoz, Antonio,López-Arza, Vicente,Langa, Fernando
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p. 5821 - 5826
(2007/10/03)
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- An improved synthesis of 1,2,4-triazoles using Ag2CO3
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An improved synthesis of 1,3,5-trisubstituted 1,2,4-triazoles via Ag2CO3 mediated cyclization of triazenes has been developed. This approach is flexible and compatible with a wide range of functional groups. The reaction was complete within 3 h and the products were isolated in moderate to high yields. The influence of the β-substituents of the amines on the triazole formation was also studied. (C) 2000 Elsevier Science Ltd.
- Paulvannan,Chen, Tao,Hale, Ron
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p. 8071 - 8076
(2007/10/03)
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