A sequence of thioxotetrahydropyrimidenes derivatives, N-(4-chloro/methoxyphenyl)-3-formyl-6-methyl-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamides (4a-l) were synthesized by the formylation of N-(4-chloro/methoxyphenyl)-6-methyl-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamides (3a-l) by dry dimethyl formamide (DMF) and phosphorous oxychloride at room temperature. Formerly, compounds (3a-l) were synthesized by the condensation of N-(4-chloro/methoxyphenyl)-3-oxobutanamide (1), various aromatic aldehydes (2a-f) and thiourea with catalytic amount of concentrated hydrochloric acid under reflux temperature. The structures of the synthesized various thioxotetrahydropyrimidenes have been characterized by using elemental analysis, Infrared, ¹H-NMR, ¹³C-NMR spectroscopy and further supported by Mass spectroscopy. All the products have been screened for their in-vitro biological assay like antibacterial activity towards Gram-positive and Gram-negative bacterial strains and antifungal activity towards Aspergillus niger at a concentration of 40 µg/ml. It was showing that the compounds 4a, 4e, 4g, 4h, 4i and 4l displayed inspirational antibacterial and antifungal activity compared to the used reference standard.

3-aryl-6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines were obtained with good yields (81-95%) via the heterocyclization reaction of 1-phenyl-2-((5-aryl-1,3,4-oxadiazole-2-yl)thio)ethane-1-ones in acetic acid. The physicochemical characteristics of the synthesized compounds were established, the structures were confirmed by the data of IR, ¹H and ¹³C NMR spectra, as well as the results of X-ray diffraction analysis. The cytotoxic, antibacterial and antifungal properties of these compounds were evaluated. In vitro screening results showed that compounds 8, 9 and 12 significantly inhibit (54-65%) the growth of HeLa, HBL-100 and CCRF-CEM cancer cell lines. It was found that the cytotoxicity of the synthesized compounds increases in the series of oxadiazoltiones (1-4) - S-derivatives (5-8) - triazolothiadiazines (9-12). Compounds 5-16 do not exhibit antimicrobial properties.

Novel 2,4-disulfonylsubstituted 5-aminothiazoles were synthesized and their anticancer activity was assessed at a high dose (10 μM) against NCI 60 cancer cell lines. Compounds 24 and 25 showed the antiproliferative activity with mean growth inhibition about 66.0%. Replacing 4-hydroxypiperidine 24 with the more hydrophilic N-methyl piperazine 25 increased the number of sensitive cell lines while replacing these hydrophilic groups with lipophilic ones abolished the anticancer activity. The COMPARE analysis showed that the tested compounds had a moderate positive correlation with alkylating agents (CCNU and methyl CCNU) and with a purine nucleotide biosynthesis inhibitor analog (L-cysteine). The results indicate that the above mechanisms of antitumor action of standard compounds are not the main ones for the tested compounds due to the lack of a high correlation. The results of this study allow us to consider compounds 24 and 25 as a basis for their further functionalization to obtain more active compounds.

This study focuses on the efficient synthesis of series of substituted 4-amino-6-(1H-benzimidazol-2-ylsulfanyl) benzene-1,3-dicarbonitrile derivatives synthesized from aldehydes, propanedinitrile, substituted thiols and catalyzed by ZnO nanoparticles (ZnONPs). All the synthesized compounds have been characterized using different spectroscopic techniques such as FT-IR, ¹H-NMR, C¹³-NMR and Mass. The compounds were evaluated for potential pharmacological applications, including antimicrobial, α-amylase inhibitory and anticancer activities. Computational calculations, DFT, in-silico molecular docking, and ADME-toxicologystudies were performed. ADMET studies indicated that all synthesized compounds adhered to Rule of five with good bioavailability. This research underscores the promising pharmacological prospects of the synthesized newbenzimidazole derivatives.

NiO cellulose nanocomposite (NiO-CN) were synthesized by the precipitation method and characterized by X-Ray diffraction (XRD), Transmission Electron Microscope (TEM), Scanning Electron Microscope (SEM), Energy Dispersive X-ray (EDX) analysis, Fourier transform infrared (FTIR) measurements and UV–vis spectroscopy. The particles obtained have an average size of 20-30 nm as shown by TEM analysis. Fourier transform infrared (FTIR) measurements were carried out to identify the possible biomolecules responsible for the capping and stabilization of the nickel oxide nanoparticles synthesized by milk. The presence of elements in the nanoparticles was also analysed by Energy Dispersive X-ray (EDX) analysis. The results of EDX analysis show the weight percentages of C, O, Ni, and N-elements in the synthesized material were 41.65%, 52.49%, 3.81%, and 2.06%, respectively. Scanning Electron Microscope (SEM) has been used to assess the morphology of the nanoparticle. The effects of NiO-cellulose nanocomposite are screened for biological activities like, antibacterial activity was done by the Disc diffusion method. The bacterial organisms used in this study were Bacillus subtilis, Salmonela abony, Staphylococcus aureus and Escherichia coli. The observed inhibition zone for these microorganisms was found to be a minimum of 3.0 mm and a maximum of 22.0 mm. Moreover, This NiO-CN also decreases the 50% load of Leishmania donovani via MTT assay with 25µg/ml concentration after 72 hours incubation.

Sulfated tungstate efficiently catalyzes the cyclodehydration of 1-(2-hydroxyphenyl)-3-aryl-1,3-propanediones to flavones under solvent-free conditions. Utilization of conventional heating, simple reaction conditions, short reaction time, ease of product isolation and purification makes this manipulation very interesting from an economic and environmental perspective. Under these conditions, twelve examples were obtained with good yields (85-94%).

A famous cisplatin anticancer agent is one of the most widely used chemotherapeutics for treating several human solid tumors. Toxicity of the normal cell is a life-threatening issue that restricts the therapeutic potential of cisplatin complex as an anticancer drug. Even though every year thousands of cisplatin-based analogs have been prepared, screened, and reported, only very few compounds entered the medical trials. Hence, new research work is still sensible. In the last few years, many mononuclear and polynuclear platinum complexes have been considerably investigated, in vitro and in vivo studies evaluated, with some compounds demonstrating significant anticancer potential. In this review, various mono-metallic and poly-metallic platinum‐based complexes with various derivatives used as ligands that have anticancer potential are defined and numerous typical examples are discussed briefly. Present investigation, numerous mononuclear cisplatin derivatives exhibited greater anticancer potency than the parent cisplatin drug. However, polynuclear cisplatin derivatives showed much better anticancer activity than mononuclear cisplatin analogs against various cancer cell lines.

The aim of this study was to investigate the modifications of the mechanical properties of polypropylene (PP) by incorporating elastomers, while considering the impact on its stiffness. Specifically, the research focused on determining the optimal loading of elastomer to achieve desirable properties and exploring the influence of these processes on the morphology and mechanical behavior of the prepared blends. Thermoplastic elastomers (TPEs) consisting of polypropylene and natural rubber (PP/NR) were prepared using a melt-mixing process, and the mechanical properties of the blends were evaluated. The stress-strain properties of the blends revealed a successful modification of PP, transforming it from a stiff and strong thermoplastic into a stiff and tough thermoplastic elastomer when 10% NR was included in the PP matrix. As the loading of NR increased, a reduction in tensile strength (TS) and modulus (E) of the blends was observed, while elongation at break (EB) increased. The flexural strength of unmodified PP was 45.9 MPa, which decreased with increasing NR loading. Similarly, the impact strength of unmodified PP was 25.8 KJ/m², whereas the values for 10%, 20%, 30%, and 40% NR inclusion were 30.8, 24.3, 20.6, and 15.2 KJ/m², respectively. The melt flow index (MFI) of unmodified PP was 14.1 g/10 min, while the values for 10%, 20%, 30%, and 40% NR inclusion were 19.4, 15.7, 11.6, and 10.2 g/10 min, respectively. The best combination of mechanical properties was observed at 10% NR inclusion in the PP matrix. The micrograph of the blends, as observed from SEM micrographs, supported the modification of PP, resulting in the production of TPE with observable adhesion sites, indicating good compatibility between the components. In a nutshell, a significant 47% increase in impact strength was achieved through the modification process.

The leaching of two pesticides, cholantraniliprole (CAP) and bispyribac-sodium (BPS) in sandy clay loam soil (soil A) and sandy loam soil (soil B) were examined, by soil columns under laboratory conditions. In addition, the effect of adding 5% biochar and wheat straw to the soils on the leaching of CAP and BPS was studied. It is clear from the results that BPS is more leachable than CAP in all soil columns, and more leached to soil B. It was found that the addition of biochar and wheat straw has a significant effect on the movements of these pesticides and can be used to reduce the environmental impact. For CAP, 71 to 97% and 84 to 97% were recovered from the soil A columns and soil B columns, respectively, while for BPS, 94 to 99% were recovered from columns of soil A and soil B.

Rhodanines are recognized as privileged heterocycles in medicinal chemistry. The main achievements include the development of drug-like molecules with numerous biological activities as well as approved drugs. The Furan nucleus is considered one of the promising heterocyclic cores in medicinal chemistry that showed numerous ranges of activity. The combination of several heterocycles in a one molecule commonly provides much more interest in the enhanced activity profile of its analogs than their parent separate constituents. Such conjugates are promising objects for modern medicinal chemistry. In this review paper recent advances in the synthesis and biological activities rhodanine-furan conjugates which its application in the different field of drug discovery.