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Disruption of the redox balance in the body causes oxidative stress that can initiate many diseases. While antioxidants reduce the level of oxidizing compounds in the medium, prooxidants promote the opposite process and have been used in therapies in particular those of cancer diseases. In this study, a series of azolyl lactones, were tested in human serum as a biological matrix and the obtained values of their oxy scores (OS) were compared. The antioxidative properties of these compounds were also tested under conditions of induced oxidative stress using an external prooxidant, t-butylhydroperoxide. The results showed that the sulphur analogue 4-azolyl coumarin 5 has the best antioxidant properties (OS –2.2), while the halogenated derivatives of pyrazolylcoumarin 7 and 8 act as prooxidants, but successfully resist oxidative stress (OS 2.7 and 2.0, respectively). Related phthalides and isocoumarins showed prooxidative properties, but azolyl isocoumarins 10 and 11 show the strongest resistance to oxidative stress, reflected in their negative oxy score value (OS –2.1 and –1.1, respectively). The results demonstrated that combining two pharmacophores with known redox properties can produce potent compounds in both directions, with the antioxidative and the prooxidative characteristics.

In the continuation of our study of substituted isocoumarins a series of novel 3-azolyl isocoumarin and their thio derivatives, including some related lactone compounds was prepared and biologically profiled against C. albicans showing moderate activity with MIC values in range of 4–60 g mL-1, in general. The additional characterisation of selected compounds was carried out by exploring their activity on CYP3A4 and CYP2D6 enzymes, while experiments on mutagenicity were performed by AMES test. The representative isocoumarins 3b, 4a and 4b showed lower inhibitory activity on CYP enzymes, when compared to the reference inhibitors, ketoconazole and quinidine. Compound 4a showed a higher mutagenic potential than the other two compounds. Further characterization included cytotoxicity profiling against normal MRC5 cells.

Pd-catalysed arylation–acetoxylation cascade, a previously reported methodology, was applied in the functionalisation of unsymmetrical dienes. Both explored classes of compounds, isoquinoline and β-carboline-derived dienes, afforded single regioisomers. Although further improvements of the process are necessary, primarily due to lower yields, the described functionalisation of the studied compounds might be useful in the synthesis of emetine and related naturally occurring compounds. [Project of the Serbian Ministry of Education, Science and Technological Development, Grant no. 172009]

A novel and efficient synthetic route has been developed for the preparation of protoberberine derivatives. The methodology designed to control, primarily, substitution patterns on the terminal rings, was used to access a small array of these compounds. Initial biological profiling suggested anticancer potential of synthesised derivatives while structure-based target fishing has identified their potential targets and has established rational basis for further structural modifications. Although the activities need further improvement, our study demonstrated that the described approach may be useful in the discovery of the novel lead compounds. [Projekat Ministarstva nauke Republike Srbije, br. 172009 i br. 175011]

The May floods in 2014 affected a large number of rural households in the vicinity of the town of Kraljevo. The flood affected a large number of villages that are located along the river West Morava and villages along the river Godačica. It was necessary to analyze the microbiological and physical chemical quality of drinking water, in order to see the impact of the May floods on the quality of drinking water rural water flooded the city, for the protection of human health, water supply and the ecosystem in general. This paper presents the results of a project which was implemented by the city of Kraljevo and funded humanitarian organization ADRA (Adventist Development and humanitarian organizations). The results of microbiological and physical chemical analysis of drinking water are shown, whose maximum allowable values are given in Regulation on hygienic quality of drinking water Fig. FRY, No.42 / 98 and 44/99 [1]. Upon the approval of funds for drinking water samples, which were tested in the laboratories of the Institute of Public Health of Kraljevo, were sampled in September and October 2014 in eight flooded villages around the town of Kraljevo. The tests were based on the analysis of microbial load of the water system and the physical and chemical parameters and the preservation of water quality.

The water of the Ibar river is used for water supply and other purposes, so monitoring the water quality of the river Ibar of primary importance for the contamination of water ecosystems and protecting human health. This paper is a continuation of the monitoring of the Ibar river of Raska and Kraljevo. Last year, at the 34th international professional scientific meeting at Tara was given the impact of wastewater municipality of Raška and Baljevac the quality of the Ibar river. A goal of this paper is to show the impact of settlements from Biljanovac to Konarevo the water quality of the Ibar river. Total of 15 measurements at three measuring sites separated 50 km are presented. The Ibar river is passing both through urban areas where the industry is developed and through uninhabited places.

The electrochemical behaviour of desloratadine (DLOR) and its derivative 3-hydroxydesloratadine (3OH-DLOR) was investigated by direct current (DCP) polarography, cyclic (CV), differential pulse (DPV) and square-wave (SWV) voltammetry in Britton-Robinson (BR) buffer solutions (pH 4-11). Both compounds are reduced at mercury electrode in irreversible two electron reduction of the C=N bond of the pyridine ring in their molecules. The difference in their electrochemical behaviour was investigated, and the most pronounced distinction is observed at pH > 9, as a consequence of the deprotonation of the phenolic moiety in 3OH-DLOR molecule, yielding significant change in their reduction potentials (Ep DLOR = -1.48 V, and Ep 3OH-DLOR = -1.6 V). The observed results correlate with calculated LUMO energy levels and Hammet substituent constants (σ). Based on the difference in the reduction potential for DLOR and 3OH-DLOR, conditions for simultaneous determination these two molecules in alkaline medium were established. The best selectivity was achieved using SWV method at pH 10. The linearity of the calibration graphs were achieved in the concentration range from 1.5 × 10-6 M - 1 × 10-5 M for DLOR and 7.5 × 10-6 M - 5 × 10-5 M for 3OH-DLOR with detection limits of 2.29 × 10-7 M and 2.08 × 10-6 M, and determination limits of 7.64 × 10-7 M and 6.94 × 10-6 M, for DLOR and 3OH-DLOR, respectively. The method was checked in human plasma sample. Good response was obtained with LOD and LOQ values of 4.63 × 10-7 M and 1.54 × 10-6 M, for DLOR and 2.39 × 10-6 M and 7.97 × 10-6 M, 3OH-DLOR, respectively.