The interaction of small molecules with DNA has become the most prominent area of research for the discovery of new drugs that may be helpful in curing of the diseases. The present research work was designed to explore the interactions of 2-(2-Oxo-2-Phenylethyl)-1,2-benzisothiazol-3(2H)-one 1,1-...
Values of the standard (p° = 0.1 MPa) massic energy of combustion in oxygen, at T = 298.15 K, for (S)-(+)-3,5-Dinitro-N-(1-phenylethyl)benzamide (S+DPB) and (R)-(−)-3,5-Dinitro-N-(1-phenylethyl)benzamide (R−DPB) were measured by using an isoperibolic micro-combustion calorimeter. The calorimete...
An efficient one-pot method for the synthesis of 2-sulfanyl-3-sulfinyl(or sulfonyl)-1H-indoles from 1-isothiocyanato-2-[sulfinyl(or sulfonyl)methyl]benzenes, derived from N-[2-(chloromethyl)phenyl]formamide by an easy four-step sequence, has been developed. The products are formed via cyclizatio...
In a preliminary article, we reported the potent allosteric enhancer activity at the A1 adenosine receptor of a small series of 2-amino-3-(4-chlorobenzoyl)-4-[4-(aryl)piperazin-1-yl)methyl]thiophene derivatives bearing electron-withdrawing or electron-releasing groups at the para-position of the...
Publisher SummaryThis chapter discusses that practical synthesis of natural (aS, 7S)-colchicine and its 3-demethyl analog remain a challenge for organic chemists. Variation of the structure of colchicine has led to several possibly less toxic analogs, such as deacetylcolchicine and 3-demethylthi...
We synthesized two chemically reactive A ring modified analogs of colchicine, 2-chloroacetyl-2-demethylthiocolchicine (2-CTC) and 3-chloroacetyl-3-demethylthiocolchicine (3-CTC). Both are similar to colchicine as inhibitors of tubulin polymerization and act as competitive inhibitors of colchicin...
The synthesis of 2-amino-5-chloro-3-(trifluoromethyl)benzenethiol was achieved by hydrolytic cleavage of 2-amino-6-chloro-4-(trifluoromethyl)benzothiazole which was prepared by cyclization of 4-chloro-2-(trifluoromethyl)phenylthiourea by bromine in chloroform, the phenylthiourea was prepared by ...
A flow injection method with chemiluminescence (CL) detection is proposed for the determination of sodium 2-mercaptoethane sulfonate (MESNA), a drug often used to reduce the urotoxic effects of antineoplastic alkylating agents. The procedure is based on the reaction of the thiol with Ce(IV) in a...
Prodrugs of isoproterenol, 3-O-,4-O-diacetylisoproterenol (DAI) and 3-O-,4-O-dibenzoylisoproterenol (DBI), were tested for effects on colonic temperature in mice. Intraperitoneal injections of DAI or DBI (20, 50 and 125 μmol/kg) produced a dose-related hypothermia. Isoproterenol (125 μmol/kg) ...
The effects of 7-alkyl substitution on the reversible intercalation of the proximate carcinogen trans-3,4-dihydroxy-3,4-dihydrobenz[a]anthracene (BAD) to calf thymus DNA have been examined using time-resolved fluorescence spectroscopy. The results indicate that in 10−3 M sodium cacodylate the bi...
In the present work, the characterization of 7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethylpurine-2,6-dione (7DDMP26D) molecule was carried out by quantum chemical method and vibrational spectral techniques. The FT-IR (4000–400 cm−1) and FT-Raman (4000–100 cm−1) spectra of 7DDMP26D were recorded in ...
Enantiomers of 2,3-dihydro-1,4-benzodioxine derivatives possessing both thrombin and fibrinogen GPIIb/IIIa binding inhibitory activities were prepared from (R)- and (S)-glycidol as potential dual antithrombotic compounds. The influence of chirality and substitution pattern on thrombin inhibition...
Homogenates of rat liver transaminate phenylpyruvate (PP), as well as α-ketoglutarate (α-KG), in the presence of L-tyrosine, 3,4-dihydroxyphenylalanine (L-DOPA) or L-tryptophan. Aminotransferase activity with phenylpyruvate and DOPA, but not with tyrosine, was inhibited by excess phenylpyruvat...
We report our observations on the activity of invertase enzyme entrapped inside the reversed micelles formed by either sodium tauroglycocholate or sodium lauryl sulfate in various organic solvents, namely hexane, n-decanol, benzene and carbon tetra-chloride. In this case more than four-fold incr...
Herein, we report a facile method to synthesis copper nanoparticles (CuNPs) using fatty acid amide, N-lauryltyramine (NLTA) and hydrazine as capping and reducing agent, respectively. As prepared CuNPs aqueous solution appears brown in color and shows intense surface plasmon resonance (SPR) band ...
Liver injury is one of the hallmark features of severe dengue virus (DENV) infection since DENV can replicate in the liver and induce hepatocytes to undergo apoptosis. N-acetyl cysteine (NAC), which is a clinically-used drug for treating acetaminophen toxicity, was found to benefit patients with...
The adsorption behavior of C.I. Reactive Blue 2, C.I. Reactive Red 4, and C.I. Reactive Yellow 2 from aqueous solution onto activated carbon was investigated under various experimental conditions. The adsorption capacity of activated carbon for reactive dyes was found to be relatively high. At p...
Dyeing of knitted cotton goods in the industry has been mostly with reactive dyes. Handling of salt laden coloured effluent arising out of dyeing process is one of the prime concerns of the industry. Cationization of cotton is one of the effective alternative to overcome the above problem. But f...
In present study, the potential of duckweed (Lemna minor L.) for degradation of an azo dye C.I. Acid Blue 92 (AB92) has been investigated. The effect of operational parameters such as initial dye concentration, pH, temperature and amount of plant on the efficiency of biological decolorization pr...
The degradation of the copper-phthalocyanine dye Reactive Blue 15 dye in sulfate medium has been comparatively studied by electrochemical oxidation with electrogenerated H2O2 (EO-H2O2), electro-Fenton (EF) and photoelectro-Fenton (PEF). Experiments with 100 cm3 solutions of 0.203 mmol dm−3 dye w...
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