Background: Imidazo[2,1-b]thiazole scaffolds were reported to possess various pharmaceutical activities. Results: The novel compound named methyl-2-(1-(3-methyl-6-(p-tolyl)imidazo[2,1-b]thiazol-2-yl)ethylidene)hydrazine-1-carbodithioate 3 acted as a predecessor molecule for the synthesis of new thiadiazole derivatives incorporating imidazo[2,1-b]thiazole moiety. The reaction of 3 with the appropriate hydrazonoyl halide derivatives 4a–j and 7–9 had produced the respective 1,3,4-thiadiazole derivatives 6a–j and 10–12. The chemical composition of all the newly synthesized derivatives were confirmed by their microanalytical and spectral data (FT-IR, mass spectrometry, 1H-NMR and 13C-NMR). All the produced novel compounds were screened for their anti-proliferative efficacy on hepatic cancer cell lines (HepG2). In addition, a computational molecular docking study was carried out to determine the ability of the synthesized thiadiazole molecules to interact with active site of the target Glypican-3 protein (GPC-3). Moreover, the physiochemical properties of the synthesized compounds were derived to determine the viability of the compounds as drug candidates for hepatic cancer. Conclusion: All the tested compounds had exhibited good anti-proliferative efficacy against hepatic cancer cell lines. In addition, the molecular docking results showed strong binding interactions of the synthesized compounds with the target GPC-3 protein with lower energy scores. Thus, such novel compounds may act as promising candidates as drugs against hepatocellular carcinoma.
Developing heterogeneous catalyst using chitosan (CS) and magnetic Fe3O4 as support has been remarkably attractive due to their availability, low cost and non-toxicity. In this work, a heterogeneous catalyst (denoted as Fe3O4@CS@MS@Ag) was fabricated by the deposition of silver nanoparticles on magnetic chitosan via an easy and facile modification of its surface with methyl salicylate (MS). The catalyst was characterized using Fourier transform infrared (FTIR) spectroscopy, thermogravimetric analysis (TGA), X-ray diffractometer (XRD), scanning electron microscopy (SEM) and energy dispersive X-ray spectroscopy (EDX). To the best of our knowledge, for the first time, CS decorated Fe3O4 (Fe3O4@CS) has shown the catalytic activity for the reduction of 4-nitrophenol (4-NP) to 4-aminophenol (4-AP) in presence of NaBH4. Surface modified magnetic chitosan (Fe3O4@CS@MS) also acts as active catalyst towards the reduction of 4-NP. However, catalytic efficiency has increased fourfold when silver-nanoparticles-deposited magnetic chitosan (Fe3O4@CS@MS@Ag) used as our target catalyst. The catalyst was separated with external magnet after each cycle of catalytic reaction and reused effectively five times with almost 90% efficiency.
In this study, a new synthetic 1,2,3-triazole-containing disulfone compound was derived from dapsone. Its chemical structure was confirmed using microchemical and analytical data, and it was tested for its in vitro antibacterial potential. Six different pathogenic bacteria were selected. MICs values and ATP levels were determined. Further, toxicity performance was measured using MicroTox Analyzer. In addition, a molecular docking study was performed against two vital enzymes: DNA gyrase and Dihydropteroate synthase. The results of antibacterial abilities showed that the studied synthetic compound had a strong bactericidal effect against all tested bacterial strains, as Gram-negative species were more susceptible to the compound than Gram-positive species. Toxicity results showed that the compound is biocompatible and safe without toxic impact. The molecular docking of the compound showed interactions within the pocket of two enzymes, which are able to stabilize the compound and reveal its antimicrobial activity. Hence, from these results, this study recommends that the established compound could be an outstanding candidate for fighting a broad spectrum of pathogenic bacterial strains, and it might therefore be used for biomedical and pharmaceutical applications.
Four new complexes derived from adamantly containing hydrazone (APH) ligand with Cu(II) (1), Co(II) (2), Ni(II) (3) and Zn(II) (4), have been synthesized and characterized using different physicochemical methods. The structure of the ligand APH and its copper complex 1 have been established by single-crystal X-ray diffraction direct methods, which reveal that complex 1 has distorted square-pyramidal geometry. Complexes 1–4 are screened against seven human cancer cell lines namely, breast cancer cell lines (MCF7, T47D, MDA-MB-231), prostate cancer cell lines (PC3, DU145) and the colorectal cancer cell line Coco-2, for their antiproliferative activities. Complex 1 has shown a promising anticancer activity compared to the other ones. The structural and spectroscopic analysis of APH and its complexes are confirmed by DFT calculations.
The present work describes the deposition of two zeolite films, sodalite and faujasite, by the hydrothermal method to tune the mesopores of clay support, which are prepared from a widely available clay depot from the central region of Morocco (Midelt). The clay supports were prepared by a powder metallurgy method from different granulometries with activated carbon as a porosity agent, using uniaxial compression followed by a sintering process. The 160 µm ≤ Φ ≤ 250 µm support showed the highest water flux compared to the supports made from smaller granulometries with a minimum water flux of 1405 L.m−2·h−1 after a working time of 2 h and 90 min. This support was chosen for the deposition of sodalite (SOM) and faujasite (FAM) zeolite membranes. The X-ray diffraction of sodalite and faujasite showed that they were well crystallized, and the obtained spectra corresponded well with the sought phases. Such findings were confirmed by the SEM analysis, which showed that SOM was crystalized as fine particles while the FAM micrographs showed the existence of crystals with an average size ranging from 0.53 µm to 1.8 µm with a bipyramidal shape and a square or Cubo octahedral base. Nitrogen adsorption analysis showed that the pore sizes of the supports got narrowed to 2.28 nm after deposition of sodalite and faujasite. The efficiencies of SOM and FAM membranes were evaluated by filtration tests of solutions containing methyl orange (MO) using a flow loop, which were developed for dead-end filtration. The retention of methylene orange (MO) followed the order: SOM > FAM > 160 µm ≤ Φ ≤ 250 µm clay support with 55%, 48% and 35%, respectively. Size exclusion was the predominant mechanism of filtration of MO through SOM, FAM, and the support. However, the charge repulsion between the surface of the membrane and the negatively charged MO have not been ruled out. The point of zero charge (pzc) of the clay support, SOM and FAM membrane were pHpzc = 9.4, pHpzc = 10.6, and pHpzc = 11.4, respectively. Filtrations of MO were carried out between pH = 5.5 and pH = 6.5, which indicated that the surface of the membranes was positively charged while MO was negatively charged. The interaction of MO with the membranes might have happened through its vertical geometry.