An Efficient Access to Pyrimidine‐based Polyfunctional Heterocycles with Anticipated Antibacterial Activity

6‐Amino‐2‐thioxotetrahydropyrimidine‐5‐carbonitrile derivative 2 was synthesized in a good yield via refluxing a mixture of arylidene 1 and thiourea in a highly basic sodium ethoxide solution. Subsequently, the synthesized pyrimidine‐2‐thione derivative 2 was allowed to interact with diversified nucleophiles and electrophiles under various reaction conditions in order to have a feasible access to further new and assorted fused heterocycles. Finally, the biological activity of the newly synthesized fused pyrimidines was screened in vitro against four different Gram‐positive and Gram‐negative bacterial strains. All the developed heterocycles were adequately characterized utilizing ¹H‐NMR, ¹³C‐NMR, Fourier transform infrared, elemental analysis, and electrospray ionization–mass spectrum and tested for their antibacterial activity.     

Antioxidant and Antimicrobial Activities of Chemically-Characterized Essential Oil from Artemisia aragonensis Lam. against Drug-Resistant Microbes

This study investigated the chemical composition, antioxidant and antimicrobial activity of essential oil extracted from Artemisia aragonensis Lam. (EOA). Hydrodistillation was employed to extract EOA. Gas chromatography with flame ionization detection (GC-FID) and gas chromatography-mass spectrometry analyses (GC-MS) were used to determine the phytochemical composition of EOA. Antioxidant potential was examined in vitro by use of three tests: 2.2-diphenyl-1-picrilhidrazil (DPPH), ferric reducing activity power (FRAP) and total antioxidant capacity assay (TAC). Agar diffusion and microdilution bioassays were used to assess antimicrobial activity. GC/MS and GC-FID detected 34 constituents in the studied EOA. The major component was Camphor (24.97%) followed by Borneol (13.20%), 1,8 Cineol (10.88%), and Artemisia alcohol (10.20%). EOA exhibited significant antioxidant activity as measured by DPPH and FRAP assays, with IC₅₀ and EC₅₀ values of 0.034 ± 0.004 and 0.118 ± 0.008 mg/mL, respectively. EOA exhibited total antioxidant capacity of 7.299 ± 1.774 mg EAA/g. EOA exhibited potent antibacterial activity as judged by the low minimum inhibitory concentration (MIC) values against selected clinically-important pathogenic bacteria. MIC values of 6.568 ± 1.033, 5.971 ± 1.033, 7.164 ± 0.0 and 5.375 ± 0.0 μg/mL were observed against S. aureus, B. subtills, E. coli 97 and E. coli 57, respectively. EOA displayed significant antifungal activity against four strains of fungi: F. oxysporum, C. albicans, A. flavus and A. niger with values of 21.50 ± 0.43, 5.31 ± 0.10, 21.50 ± 0.46 and 5.30 ± 0.036 μg/mL, respectively. The results of the current study highlight the importance of EOA as an alternative source of natural antioxidant and antibacterial drugs to combat antibiotic-resistant microbes and free radicals implicated in the inflammatory responses accompanying microbial infection.     

4-Hydroxy-2-quinolones: syntheses,reactions and fused heterocycles

Molecular Diversity - The interesting pharmaceutical and biological activities of 4-hydroxy-2-quinolones make them valuable in drug research and development. Hence, many publications have recently...     

Two-machine flowshop scheduling problem with coupled-operations

This paper addresses a generalization of the coupled-operations scheduling problem in the context of a flow shop environment. We consider the two-machine scheduling problem with the objective of minimizing the makespan. Each job consists of a coupled-operation to be processed first on the first machine and a single operation to be then processed on the second machine. A coupled-operation contains two operations separated by an exact time delay. The single operation can start on the second machine only when the coupled-operation on the first machine is completed. We prove the NP-completeness of two restricted versions of the general problem, whereas we also exhibit several other well solvable cases.

     

TiO2/clay as a heterogeneous catalyst in photocatalytic/photochemical oxidation of anionic reactive blue 19

A TiO₂-coated Tunisian clay (TiO₂–clay) was synthesized by a typical impregnation method. The physicochemical characterization points to a successful impregnation of titania on the clay surface. The activity of this structured catalyst was studied in the photocatalytic/photochemical oxidation of anionic reactive blue 19 (RB 19). The effect of UVA and solar irradiation (UV-solar) was studied at room temperature. TiO₂–clay demonstrated an effective degradation of RB 19 under both types of irradiation. Moreover, in this study, the effects of various oxidants such as hydrogen peroxide (H₂O₂), potassium peroxodisulfate (K₂S₂O₈) and sodium carbonate (Na₂CO₃) were thoroughly investigated. H₂O₂ was a promising oxidant for promoting RB 19 degradation under UV_A. The kinetics of discoloration of RB 19 followed a pseudo-first-order rate law. We can remark that 20 min of UV irradiation was enough to achieve 100% discoloration of the aqueous solution. However, under UV–Vis, HPLC and chemical oxygen demand measurements indicated, that a longer reaction time (of around 45 min) was required for achieving the complete dye mineralization. The findings clearly demonstrated the applicability of this TiO₂/clay catalyst for the photocatalytic oxidation of RB 19.     

Estimation of a class of quasi‐resonances generated by multiple small particles with high surface impedances

We deal with the stationary acoustic waves propagating in a cluster of small particles enjoying high contrasts. Such contrasts allow the appearance of (complex valued) resonances that are close to the real line as the size of the particles becomes small. For single (but not necessarily small) particles, we derive the characteristic equation that generates a class of these resonances (the ones for which the corresponding eigenfunctions are uniformly constant). For multiple and small particles, we provide sufficient conditions on the contrasts that generates quasi‐resonances for which the corresponding eigenfunctions are uniformly constant. Precisely, we show that, if we distribute the particles on a uniform line, then the existence of such quasi‐resonances is related to the eigenvalues of the Harary matrix. To show these results, we take, as the small contrasted particles, small obstacles with high surface impedances λ of the form λ: = βa^?1 ? αβa^{?1 + h} where a is the maximum radi of the particles, with a < <1, and β is a universal and positive constant depending only on the shape of the particles (but not on their size). In this case, if the relative constant α is an eigenvalue of the Harary matrix, then the used frequency is a quasi resonance of the cluster of the small particles where the error of approximation is of the order for h ∈ (0,1) as a < <1.