Nitrophenyl-group-containing Heterocycles. Part I. Synthesis, Characterization, Anticancer Activity and Antioxidant Properties of Some New 5,6,7,8-tetrahydroisoquinolines Bearing 3(4)-nitrophenyl Group

Regioselective cyclocondensation of 2,4-diacetyl-5-hydroxy-5-methyl-3-(3-nitrophenyl/4-nitrophenyl)cyclohexanones 1a,b with cyanothioacetamide fforded the corresponiing 7-acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8-(3-nitrophenyl/4-nitrophenyl)-5,6,7,8-tetrahydro-soquinoline-3(2H)-thiones 2a,b in 93-96%. Reaction of compounds 2a,b ethyl iodide, 2-chloroacetamide or N-(naphthalen-1-yl)-2-chloroacetamide (5) in the presence of sodium acetate gave the corresponding p(5,6,7,8-tetrahydroisoquinolin-3-yl)thio derivatives 3a,b, 4a,b and 6a,b. In a similar manner, reaction of a,b with other N-aryl-2-chloroacetamides 7a-d gave 2-[(7-acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8-(3-nitrophenyl/4-nitrophenyl)-5,6,7,8-tetrahydroisoquinolin-3-yl)thio]-N-arylacetamides (8a-g). On heating of compounds 8a-e in ethanol containing anhydrous sodium carbonate, they converted into 7-acetyl-1-amino-N-aryl-5,8-dimethyl-8-hydroxy-6-(3-nitrophenyl/4-nitrophenyl)-6,7,8,9-tetrahydrothieno[2,3-c]isoquinoline-2-carboxamides 9a-e. Structural formulae of all synthesized compounds were characterized on the basis of their spectroscopic data. Also, the applications of most synthesized isoquinolines as anticancer and as antioxidant agents have been carried out and the obtained results are reported herein.

Effects of Four Carboxyl-Containing Additives on Imitation Gold Electroplating Cu-Zn-Sn Alloys in an HEDP System

The requirements for using noncyanide imitation gold plating as decorative electroplating are increasing; thus, continuously improving the quality of the coating of the imitation gold plating and optimizing the coating process have become the current priority. In this work, hydroxyethylidene diphosphonic acid (HEDP) was used as the main complexing agent, CuSO4·5H2O, ZnSO4·7H2O and NaSnO3·3H2O were the main salts, and NaOH and anhydrous sodium carbonate were used as the buffers to prepare the electroplating solution. Using sodium citrate (SC), sodium potassium tartrate (SS), sodium gluconate (SG), and glycerol (Gl) as four additives, the effects of the number of carboxyl groups on the properties of a Cu-Zn-Sn alloy coating were compared. The electrochemical analysis showed that Cu-Zn-Sn alloy codeposition occurred at -0.50 V vs. Hg|HgO. The scanning electron microscopy (SEM) results showed that the particle size of the coatings obtained with carboxyl-containing additives was more uniform than that obtained with the electroplating solution without additives. The X-ray fluorescence spectrometry (XRF) analysis revealed that the composition of the Cu-Zn-Sn alloy coating obtained by using SC as an additive in the electroplating solution was 89.75 wt% Cu, 9.61 wt% Zn, and 0.64 wt% Sn, and the color of the coating was golden yellow. The X-ray diffraction (XRD) pattern showed that the coating was a mixture of Cu, Cu5Zn8, CuSn, Cu6Sn5, and CuZn phases. The analysis of the electroplating solution by UV, IR and NMR spectroscopy methods indicates that the additives improve the coating by affecting the complexation reaction of metal ions. These results can provide technical and theoretical guidance for developing Cu-Zn-Sn ternary alloy electrodeposition technology with the new cyanide-free HEDP alkaline electroplating system.

Molecular Modelling Studies of 1,4-Diaryl-2-Mercaptoimidazole Derivatives for Antimicrobial Potency

Background: : Imidazoles are considered as potent antimicrobial agents. In view of this 2-mercaptoimidazoles were synthesized and evaluated for antimicrobial study. Methods:: Some new 2-mercaptoimidazoles 4a-r were synthesized using substituted aniline and substituted phenacyl bromides in the presence of anhydrous sodium carbonate or potassium carbonate and potassium thiocyanate under solvent-free conditions catalyzed by eco-friendly ptoluene sulfonic acid. Results: : The structure of compounds was evaluated on the basis of Infrared spectroscopy (IR), 1HNMR (proton nuclear magnetic resonance) and mass spectral studies. These novel compounds were screened for in-vitro antibacterial and antifungal potency against Staphyllococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. Further, the study was rationalized by molecular modeling studies. All the compounds were subjected to molecular modeling studies for inhibition of enzyme 14α-demethylase. Conclusions:: The compounds were found to be effective in inhibiting the growth of pathogens. The in-silico results depicted that, all the synthesized compounds have minimum binding energy and good affinity towards the active site and thus can be considered as good inhibitors of 14α- demethylase enzyme.

Synthesis, Characterization and Biological Activates Studies of some New Derivatives From 2-aminoo-5-mercapto-1, 3, 4-thiadiazole

In this work, thiadiazole derivatives were prepared by taking advantage of active sites in (2-amino-5-mercapto-1, 3, 4-thiadiazole) as a starting material base. The main heterocyclic compounds (1, 3, 4-thiadiazole, oxazole) etc, 2-amino-5-mercapto-1,3,4-thiadiazole compound (1) was prepared by cyclic closure of thiosemicarbazide compound with anhydrous sodium carbonate and carbon disulfide. Oxidation of (1) via hydrogen peroxide, to have (2) which was treated with chloro acetyl chloride to get (3). Preparation of thiazole ring (4) was from reacting of (3) with thiourea. Synthesis of diazonium salts (5) from compound (4) using sodium nitrite and HCl. Compound (5) reacted with different ester compounds to prepare a new azo compounds (6–8).Compound (3) reacts with viruses secondary amine to prepare compound (9–11). Full characterization of the synthesized compounds was done by using spectroscopic analysis such as FT-IR, 1H-NMR and C.H.N.S. technique.

Preparation of some azo compounds by diazotization and coupling of 2- amino -5 – thiol -1,3,4- thiadizaole

2- amino -5- thiol-1,3,4- thiadiazole (S1) was prepared by cyclic locking of thiosemicarbazide in the presence of anhydrous sodium carbonate and CS2. diazotization of (S1) compound gave diazonium salt (S2) that reacts with different activated aromatic compounds to get the following azo compounds ,2 [(4- aminophenyl) diazenyl ] 1,3,4- thiazdiazole-5- thiol (S3) ,2-[4-amino- 1-naphthyl diazenyl] -1,3,4 – thiazdiazole-5-thiol (S4) , 3-amino-4-[(5- mercapto -1,3,4- thiadiazole -2-yl) diazenyl ] phenol(S5) ,1-[(5-mercapto-1,3,4-thiadiazole-2-yl) diazenyl] -2-naphthol (S6) , 5-{[4-(dimethylamino) phenyl] diazenyl}-1,3,4-thiadiazole-2- thiol(S7) ,5-{[4-(diethylamino) phenyl] diazenyl}-1,3,4- thiadiazole-2- thiol(S8) ,2- amino-5-[(5-mercapto-1,3,4-thiadiazole-2-yl) diazenyl] phenol(S9) . All the prepared azo compounds have been characterized and identified through the study of their some physical, chemical and spectrometrical (U.V.I.R) properties.

Study on Direct Reduction of Vanadium Slag

In this paper the process of direct reduction of vanadium slag was adopted. The main factor was determined by uniform experimental design and single factor analysis, and then the optimum process condition was drawn by the test. The test results showed that the regression equation curve fitting of the experiment data was very significant, the main factors affecting the vanadium slag reduction (according to the primary and secondary order) was the content of anhydrous sodium carbonate, roasting temperature, roasting time and reduction of carbon content. The factors for the reduction of the optimum process conditions are the carbon coefficient 1.04, roasting temperature 1100°C, roasting reduction time 4h, 4% mass percent of anhydrous sodium carbonate and slag. Under the optimum conditions, the actual rate of weight loss and theory rate of weight were close to 0, the results could be reproduced, and the vanadium slag metallization rate was 75%~83%.