The synthesis is described of a series of mono-, bis-, and tris(1,3-dithiol-2-ylidene) derivatives7,9 and10 starting from 1,3-indanedione. Cyclic voltammetric data establish that the π-electron donor ability of these molecules increases in the sequence7
Several new monoalkyl-thioalkyl substituted TTF donors have been prepared via the mesoionic 2-dialkylamino-5-alkyl-1,3-dithiolium-4-thiolate 1. By S-alkylation 1 was transformed into a number of mono- and bis-1,3-dithiolium salts 6, which were coupled with the anion of 4., 5-dimethyl-2H-1,3-dith...
The poor results in the syntheses of unsymmetrically substituted TTF derivatives carried out with mono or unsubstituted diethyl 1,3-dithiol-2-yl-phosphonates is here explained by the existence of an equilibrium between the cyclic and open forms of their corresponding carbanionic salt, with possi...
The scope and limitations of the synthesis of unsymmetrically substituted TTF derivatives via the “phosphonate way” was investigated using as precursors 1,3-dithiol-2-yl-phosphonates and 1,3-dithiol-2-yliden iminium salts with various substitutents on the dithiole cycles.Except for the un- or ...
This chapter deals with the synthesis, reactivity, and characterization of five-membered heterocycles containing two sulfur atoms in positions 1 and 3 of the ring, that is, 1,3-dithiolylium ions, mesoionic 1,3-dithiol-4-ones and 4-thiones, 1,3-dithioles, and 1,3-dithiolanes. Aspects of the react...
In order to expand the arsenal of biologically active substances of anticonvulsive action by the interaction of 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)acetic acid with the corresponding amines in the presence of N,N′-carbonyldiimidazole in the dioxane medium, a systematic series of 2-(2,4-...
2,4-O-Benzylidene-l-xylose was converted via a Wittig reaction into Z-2,4-O-benzylidene-5,6-dideoxy-6-C-(2,4-dichlorophenyl)-d-xylo-hex-5-enitol (17), which, on hydrogenation, gave 5,6-dideoxy-6-C-(2,4-dichlorophenyl)-d-xylo-hexitol (33). tert-Butyldimethylsililation of the primary hydroxyl grou...
A series of 14 ethyl 1-(2,4-dichlorophenyl)-1H-pyrazole-3-carboxylates has been synthesized from the cyclocondensation reaction of ethyl 4-methoxy-2-oxoalk[cycloalk]-3-enoates [EtO2CC(O)C(R2) = C(R1)OR, where R = H, Me; R1 = Pr, Ph, 4-MeOC6H4, 4-MeC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 4-NO2C6H4, fu...
This study describes synthesis and evaluation of novel 5-Chloro-2-thiophenyl-1,2,3-triazolylmethyldihydroquinolines 7a-o as dual inhibitors of Mycobacterium tuberculosis and influenza virus. Huisgen’s [3+2] dipolar cycloaddition of 6-(azidomethyl)-5-chloro-2-(thiophen-2-yl)-7,8-dihydroquinoline...
A new derivative of 1-phenyl-3-methyl-5-pyrazolone, 4,4-dichloro-1-(2,4-dichlorophenyl)-3-methyl-5-pyrazolone, named TELIN, was chemically synthesized and identified as a potent inhibitor of human telomerase in the cell-free telomeric repeat amplification protocol. TELIN inhibited telomerase act...
SummaryEthers of 1-(2,4-dichlorophenyl)-2-(1-H-imidazolyl)ethanol bearing ramified and/or unsaturated chains have been synthesized in order to specify the role of lipophilicity or steric contributions on antifungal activity against yeast for miconazole-like structures. The presence of ramificati...
The development of novel HIV-1 NNRTIs offers the possibility of generating novel structures with increased potency. Based on the bioisosteric principle, a novel series of 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamide derivatives were designed, synthesized using a simple an...
As a part of a program to develop novel antifungal agents, new compounds which incorporate the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared. These compounds were computationally investigated to assess whether the 1,4-benzothiazine moiety was a suitable bioisost...
6-(2,4-Dichlorophenyl)-d-erythro-1,2,4-hexanetriol, synthesised from d-glucose, was partially silylated, then reacted with 2-methoxypropene to afford 1-O-tert-butyldimethylsilyl-6-(2,4-dichlorophenyl)-2,4-O-isopropylidene-d-erythro-1,2,4-hexanetriol (17). Desilylation of 17 gave 6-(2,4-dichlorop...
Pediocin PA-1 production by Pediococcus acidilactici UL5 cells immobilized in κ-carrageenan/locust bean gum gel beads was studied during repeated-cycle batch (RCB) culture with pH control in Man Rogosa and Sharpe (MRS) broth supplemented with 1% glucose and whey permeate (SWP) medium. The pedio...
The bacteriocin from Pediococcus acidilactici M, designated as Pediocin AcM, was rapidly purified to homogeneity by the pH mediated cell adsorption-desorption method and semi-preparative reversed-phase HPLC. The purification yield was 40.4% and the specific activity was increased by 2450-fold. I...
Fermentative production of bacteriocin, pediocin AcH was studied in a batch fermenter using Pediococcus acidilactici H. An initial pH of 6.5 and a fermentation temperature of 37 °C were found to be favourable for optimum production up to 20 h of fermentation time. Rate of cell growth utilizing ...
Data for the cell growth of Pediococcus acidilactici H during the fermentative production of bacteriocin, pediocin AcH (taken from a previous study) was modeled by two sigmoidal functions, modified Gompertz and Logistic. Results showed that the models could adequately account for the cell growth...
The potentiality of a native isolate, Pediococcus acidilactici C20, to produce quantifiable amounts of pediocin C20 on whey permeate was studied. The molecular basis for the presence of a β-gal like gene was shown by DNA dot-blot technique followed by β-galactosidase (β-Gal) assay on native p...
The anti-listerial effect of pediocin PA-1 and its producing strain, Pediococcus acidilactici UL5, was investigated in vivo using an ICR mouse model. The effect of intra-gastric administration of a single dose of P. acidilactici UL5 (4 × 1010 CFU/animal) on the propagation of Listeria monocytog...
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