Classical and advanced chemical sciences
A highly efficient protocol was developed for the synthesis of 3-(indoline-1-carbonyl)-N-(substituted)benzenesulfonamide compounds with excellent yields. The in vitro anticancer activity of the new 3-(indoline-1-carbonyl)-N-(substituted)benzenesulfonamide derivatives against A549 (lung cancer cell), HeLa (cervical), MCF-7 (breast cancer cell) and Du-145 (prostate cancer cell) cell lines were studied. Most of the tested compounds showed anticancer activity (IC50 values ranged between 1.98 and 9.12 μM against different cell lines).
Keywords: Indoline; sulfonamides; anticancer activity.
In order to explore the anticancer and antimicrobial activity associated with the thiazolone framework, several new (Z)-2-((5-(3-fluorobenzylidene)-4-oxo-4,5-dihydrothiazol-2-yl)amino)carboxylic acid derivatives have been synthesized in water as a solvent. All synthesized compounds were evaluated for anticancer and antimicrobial activity in vitro. Amongst these, the 3-methylbutanoic and the 3- or 4-methylpentanoic acid derivatives, the 3-hydroxy-, the 3-(1H-imidazol-4-yl) and the 3-(4-hydroxyphenyl)propanoic acid derivatives and the succinic acid derivative showed high antibacterial and antifungal activity. The unsubstituted propanoic acid derivative exhibited significant antibacterial activity against B. subtilis and significant antifungal activity against fungal strains, i.e., A. flavus. The in vitro anticancer studies revealed that the 3-(hydroxy)-, the 3-(1H-imidazol-4yl)- and the 3-(4-hydroxyphenyl)propanoic acid, or the succinic acid derivatives are the most active compounds against MCF-7 and BT-474 human breast cancer cell lines.
Keywords: 2-thioxothiazolidin-4-one, 3-fluorobenzaldehyde, amino acids, anticancer, antimicrobial
Diabetes mellitus is a chronic endocrine disorder that affects the metabolism of carbohydrates, proteins, fat, electrolytes and water. α-Amylase and α-glucosidase are the crucial enzymes required for the digestion of the carbohydrate. These enzymes play a vital role in the breakdown of starch in the diet and its activity has been correlated to postprandial blood glucose levels, the control of which is essential for maintaining the quality of life for diabetic patients. We report the synthesis, characterization and biological evaluation of new substituted 2-phenoxynicotinaldehydes as α-amylase inhibitors. A new general method based on the aromatic nucleophilic substitution reactions of 2-chloronicotinaldehyde with differently substituted phenols in the presence of K2CO3 in dry dioxane was developed to furnish the corresponding substituted 2-phenoxynicontinaldehydes with 70-80% yields.
Keywords: diabetes; α-amylase; α-glucosidase; 2-phenoxynicotinaldehydes.
Materials and environmental chemistry
The waste from coal-based thermal power plants in the form of pond ash is utilized in making of environment-friendly cement mortar with using sand and cement. The mechanical properties like compressive strength under uniaxial stress of brick masonry and cement mortars prepared with the incorporation of pond ash into the cement mortar at various mixing ratios have been determined. The mathematical relationship of compressive stress values and the composition of brick, mortar and masonry have been developed. The compressive stress, strain and Young’s modulus values and their relationships have been determined. Using pond ash lead to an increase in the strength of the mortar and brick masonry prism prepared.
Keywords: Pond ash; cement mortar; compressive strength; Young’s modulus
Chemical and biological aspects of life
Vernonia amygdalina (Del.) is widely cultivated in tropical Africa and known for its bitter principles. The extracts of this plant are used in folklore medicine to treat fevers, measles, tuberculosis, toothaches, parasitic infections, asthma, diarrhoea and in managing diabetes mellitus. The growing concerns arising from the treatment and management of the diabetes prompted this study. Hence, the hypoglycaemic potentials of leaf, stem and root (squeezed and methanolic) extracts of the plant were investigated in normo-glycaemic and alloxan-induced rats. The blood glucose levels in normal and diabetic rats were determined after the administration of 300mg/kg of extract and 150mg/kg of alloxan monohydrate at time (t) = 0, 1, 2 and 4 h. The hypoglycaemic activities of the squeezed extracts of leaves, stem and roots were not significant in both normal and diabetic rats. However, the methanolic extracts of the leaves and roots demonstrated significantly remarkable hypoglycaemic activities compared with the activity given by the stem extract. The methanolic extracts of leaves and root have shown to be effective in lowering blood glucose level (80% reduction after 4h) while the stem afforded a poorly 20% reduction after 4 h. The results from this study have lent scientific credence to the ethnobotanical use of the plant in the treatment and management of diabetes mellitus. However, the claims that the stem is as effective in the herbal therapy of this metabolic disease can not be supported by the results obtained from this study.
Keywords: Normo-glycaemic; alloxan; extracts; diabetes mellitus; hypoglycaemic
Industrial and engineering chemistry, biotechnology
Production of metakaolin to increase the properties of cement and mortar has been studied from ordinary multicomponent mineral clays and shales as cheap raw materials. Alluvium clay shales formed as a result of mudflows were used as starting material and the optimal mode of its heat treatment has been elaborated to obtain the maximal amount of metakaolin. The pozzolanic properties of the heat-treated clay shales were monitored with making and testing various types of cement.
Keywords: metakaolin; portland cement; shales; pozzolanic admixture; heat treatment
Theoretical and computational chemistry
Novel semiconductor-base nanotechnology is gradually moving into new applications in the world economy. Semiconductor application requires increasing of investigations in the direction of their properties. The primary criterion of semiconductor suitability for use in semiconductor devices is its electrical properties, particularly current carriers mobility. Therefore, the problem connected with the explanation of the experimental results of current carriers mobility on the base of theoretical formulas is very urgent. In the present paper current carriers mobility due to ionized impurity scattering is discussed and calculated using numerical methods. Calculations have been done for different temperatures and different range of current carriers concentration in InAs.
Keywords: semiconductor, current carriers mobility, impurity ions, numerical calculations