A novel series of carbamothioylamino-benzene-sulfonamidethiophene-carboxylates 4a-c and thieno [3,2-d]pyrimidin-2-yl-amino-benzene-sulfonamides 5a-c were synthesized in a series of synthetic steps and were used as key intermediates for the synthesis of thienotriazolopyrimidine-benzene-sulfonamide derivatives 6a-c and 7a-c. Thieno[3,2-d]pyrimidinones (8 and 9) were also prepared. Compound 9 was used as an intermediate for the synthesis of imidazole/1,2,4-triazole and tetrazine functionalized thieno[3,2-d]pyrimidine derivatives (10-12). Pyrrole derivatives/pyrrolopyrimidine/pyrrolotriazolopyrimidine functionalized thiophenes (15-19) were also synthesized. Structures of the newly synthesized compounds were established by elemental analysis and spectral data. Most of the newly synthesized compounds were evaluated for their in vitro activity against three human tumor cell lines, namely, liver cancer (HepG-2), colon cancer (HT-29) and lung cancer (NCI-H460), using doxorubicin as standard. , resp.) showed higher activity against all cell lines than doxorubicin. Most of the compounds were also screened for antibacterial activity using ciprofl oxacin as standard drug. Compounds 4b and 6b, both containing benzenesulfonamide linked to N-, 10 bearing imidazole moiety, and 15 and 19b,c with a thiophene-2-carboxylic acid chain, exhibited high activity against Gram-positive and Gram-negative bacteria.
The Pipper nigram (P. nigram) leaf extract was used for the biosynthesis of copper oxide nanoparticles (CuO NPs) and the successful formation of the resultant product was confirmed through several physicochemical techniques. The chemical structure and the elemental composition were analysed through Fourier transform infrared (FTIR) and energy dispersive X-ray (EDX) spectroscopies, respectively. The crystalline structure and crystallite size were investigated through an X-ray diffractometer (XRD) and a monoclinic crystallite with a size of 40.68 nm was reported. Even-distributed particles with an average particle size of 49.75 nm were seen in the scanning electron micrograph (SEM), whereas the thermal stability was checked during the thermogravimetric analysis (TGA). The ultra-violet and visible (UV-Visible) spectroscopy was operated to study the light absorbance phenomena and to determine the band gap energy from the absorption edge, which was found to be 1.47 eV. The CuO NPs were used as antibacterial agents against gram-negative bacteria (GNB) and gram-positive bacteria (GPB), and greater inhibition zones were seen against the former one. The antioxidant test was also carried out against 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals and the antioxidant potential of CuO NPs was found to be higher than ascorbic acid.
Centaurea parviflora (C. parviflora), belonging to the family Asteraceae, is an Algerian medicinal plant used in folk medicine to treat different diseases related to hyperglycemic and inflammatory disorders, as well as in food. The present study aimed to assess the total phenolic content, in vitro antioxidant and antimicrobial activity and phytochemical profile of the extracts of C. parviflora. The extraction of phenolic compounds from aerial parts was conducted using solvents of increasing polarity starting from methanol, resulting in crude extract (CE), to chloroform extract (CHE), ethyl acetate extract (EAE) and butanol extract (BUE). The total phenolic, flavonoid and flavonol contents of the extracts were determined using the Folin–Ciocalteu and AlCl3 methods, respectively. The antioxidant activity was measured with seven methods: 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, galvinoxyl free-radical-scavenging test, 2,2′-Azino-Bis(3-Ethylbenzothiazoline-6-Sulfonic Acid) (ABTS) assay, cupric reducing antioxidant capacity (CUPRAC), reducing power, Fe+2-phenanthroline reduction assay and superoxide-scavenging test. The disc-diffusion method aimed at testing the sensitivity of bacterial strains toward our extracts. A qualitative analysis with thin-layer chromatography of the methanolic extract was performed. Moreover, HPLC-DAD-MS was used to establish the phytochemical profile of the BUE. The BUE was found to contain high amounts of total phenolics (175.27 ± 2.79 µg GAE/mg E), flavonoids (59.89 ± 0.91 µg QE/mg E) and flavonols (47.30 ± 0.51 µg RE/mg E). Using TLC, different components such as flavonoids and polyphenols were noted. The highest radical-scavenging ability was recorded for the BUE against DPPH (IC50 = 59.38 ± 0.72 µg/mL), galvinoxyl (IC50 = 36.25 ± 0.42 µg/mL), ABTS (IC50 = 49.52 ± 1.54 µg/mL) and superoxide (IC50 = 13.61 ± 0.38 µg/mL). The BUE had the best reducing power according to the CUPRAC (A0.5 = 71.80 ± 1.22 μg/mL), phenanthroline test (A0.5 = 20.29 ± 1.16 μg/mL) and FRAP (A0.5 = 119.17 ± 0.29 μg/mL). The LC-MS analysis of BUE allowed us to identify eight compounds including six phenolic acids and two flavonoids: quinic acid, five chlorogenic acid derivatives, rutin and quercetin 3-o-glucoside. This preliminary investigation revealed that the extracts of C. parviflora have a good biopharmaceutical activity. The BUE possesses an interesting potential for pharmaceutical/nutraceutical applications.
Staphylococcus aureus (S. aureus) is a serious infection-causing pathogen in humans and animal. In particular, methicillin-resistant S. aureus (MRSA) is considered one of the major life-threatening pathogens due to its rapid resistance to several antibiotics in clinical practice. MRSA strains have recently been isolated in a number of animals utilized in food production processes, and these species are thought to be the important sources of the spread of infection and disease in both humans and animals. The main objective of the current study was to assess the prevalence of drug-resistant S. aureus, particularly vancomycin-resistant S. aureus (VRSA) and MRSA, by molecular methods. To address this issue, a total of three hundred samples (200 meat samples from cattle and sheep carcasses (100 of each), 50 hand swabs, and 50 stool samples from abattoir workers) were obtained from slaughterhouses in Egypt provinces. In total, 19% S. aureus was isolated by standard culture techniques, and the antibiotic resistance was confirmed genotypically by amplification nucA gen. Characteristic resistance genes were identified by PCR with incidence of 31.5%, 19.3%, 8.7%, and 7% for the mecA, VanA, ermA, and tet L genes, respectively, while the aac6-aph gene was not found in any of the isolates. In this study, the virulence genes responsible for S. aureus’ resistance to antibiotics had the highest potential for infection or disease transmission to animal carcasses, slaughterhouse workers, and meat products.
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