Based on the extensive biological activities of thiazole derivatives against different types of diseases, we are interested in the effective part of many natural compounds, so we synthesized a new series of compounds containing di-, tri- and tetrathiazole moieties. The formation of such derivatives proceeded via reaction of 2-bromo-1-(4-methyl-2-(methylamino)thiazol-5-yl)ethan-1-one with heterocyclic amines, o-aminothiophenol and thiosemicarbazone derivatives. The structure and mechanistic pathways for all products were discussed and proved based on spectral results, in addition to conformational studies. Our aim after the synthesis is to investigate their antimicrobial activity against various types of bacteria and fungi species. Preceeding such an investigation, a molecular docking study was carried out with selected conformers, as representative examples, against three pathogen-proteins. This preliminary stage could support the biological application. The potency of these compounds as antimicrobial agents has been evaluated. The results showed that derivatives which have di- and trithiazole rings displayed high activity that exceeds the used standard antibiotic.

Application of triazoles in the development of microtubule targeting agents.

Aflatoxins (AFs) are a family of fungal toxins that produced in food and feed by two Aspergillus species (Aspergillus flavus and Aspergillus parasiticus). Several techniques have been reported for AFs detection including high-pressure liquid chromatography, enzyme-linked immunosorbent assay, surface plasmon resonance and recombinant immune blotting assay. But, these methods are disadvantaged because they consumed a long time for analysis; in addition, they required a piece of complicated and expensive equipment. Therefore, developing of inexpensive sensors with high selectivity and sensitivity for detecting of AFs levels without extensive sample preparation has received great attention. Several electrochemical AFs sensors have been reported; however, there is still a need for developing a new, simple and rapid electrochemical AFs sensor. Here, we have developed a new AFs sensor based on Au nanostructures/graphene nanosheets modified ITO substrate that could enhance the Raman effect and the electrochemical conductivity. The modified electrode was prepared based on layer-by-layer electrochemical deposition method. AFs antibody was immobilized onto the Au nanostructures/graphene nanosheets; then it was used as a probe for rapid, simple and cheap detection of AFs level using Raman spectroscopy and electrochemical techniques. Our results demonstrated that the developed system showed a simple, easy and sensitive sensor for monitoring low concentrations of AFB1 with a detection limit of about 6.9 pg/mL, also it allowed the determination of AFB1 in spiked food samples.

Hepatocellular carcinoma is a highly aggressive and difficult-to-treat type of cancer. Incorporating urea functionality into the backbone of organoselenium compounds is expected to develop promisin... Graphical abstract

Four pyrazolone derivatives and their corresponding silver complexes were synthesized and characterized. Based on elemental analysis, 1 : 2 (M : L) molar ratio was suggested for all inspected complexes. ¹H, ¹³C NMR, mass, UV-Vis, TGA, and IR were the spectral tools used for describing the formulae. Moreover, XRD patterns and SEM pictures were used to evaluate the particle sizes which appeared strongly in nanometer range. CT-DNA study is the major consideration in this study, to test the interacting ability of all synthesized cationic complexes towards cell DNA. Each binding constant was computed and correlated with the Hammett sigma constant. Antitumor activity was examined upon three carcinoma cell lines (MCF-7, HepG2, and HCT116). The high efficiency was recorded towards MCF-7 (breast carcinoma) cell line. Kinetic studies yield essential parameters to assert on the rule of metal atom on thermal feature of organic compounds. Molecular modeling was implemented to optimize the structures of compounds. Also, molecular docking was achieved to obtain a clear view about proposed drug behavior within the affected cells. This was achieved through comparing the calculated internal energy values of all docking complexes. All the tested compounds displayed a significant interaction with breast cancer protein (strong matching with practical result) followed by DNA polymerase protein.