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45 result(s) for "Karam, Eman A."
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Synthesis, Docking Studies, and In Vitro Evaluation of Some Novel Thienopyridines and Fused Thienopyridine–Quinolines as Antibacterial Agents and DNA Gyrase Inhibitors
A series of novel thienopyridines and pyridothienoquinolines (3a,b–14) was synthesized, starting with 2-thioxo-1,2-dihydropyridine-3-carbonitriles 1a and 1b. All compounds were evaluated for their in vitro antimicrobial activity against six bacterial strains. Compounds 3a,b, 4a, 5b, 6a,b, 7a, 9b, 12b, and 14 showed significant growth inhibition activity against both Gram-positive and Gram-negative bacteria compared with the reference drug. The most active compounds (4a, 7a, 9b, and 12b) against Staphylococcus aureus were also tested for their in vitro inhibitory action on methicillin-resistant Staphylococcus aureus (MRSA). The tested compounds showed promising inhibition activity, with the performance of 12b being equal to gentamicin and that of 7a exceeding it. Moreover, the most promising compounds were also screened for their Escherichia coli DNA gyrase inhibitory activity, compared with novobiocin as a reference DNA gyrase inhibitor. The results revealed that compounds (3a, 3b, 4a, 9b, and 12b) had the highest inhibitory capacity, with IC50 values of 2.26–5.87 µM (that of novobiocin is equal to 4.17 µM). Docking studies were performed to identify the mode of binding of the tested compounds to the active site of E. coli DNA gyrase B.
New Quinazolin-4(3H)-one Derivatives Incorporating Hydrazone and Pyrazole Scaffolds as Antimicrobial Agents Targeting DNA Gyraze Enzyme
The present work includes the synthesis of a new series of quinazolin-4(3H)-one compounds (4a–f, 5a–d) as antimicrobial agents. The starting compound, 2-hydrazinylquinazolin-4(3H)-one (2), was synthesized and treated with different carbonyl compounds to afford the hydrazone derivatives 4a–f. In addition, the hydrazone derivatives 4a–d were treated with a DMF/POCl3 mixture to give the formyl-pyrazole derivatives 5a–d. All the target compounds were evaluated as antimicrobial agents against four bacterial and four fungal strains. The majority of the tested compounds showed potent antimicrobial activity compared with the reference antibiotics. The most potent antimicrobial activity was shown by 5a with MIC values in the range (1–16) μg/mL. In addition, the most potent compounds against E. coli were evaluated for their inhibitory activity against E. coli DNA gyrase, whereas the target compounds 4a, 5a, 5c, and 5d showed the most potent inhibition to the target enzyme with IC50 values ranging from 3.19 to 4.17 µM. Furthermore, molecular docking studies were performed for the most active compounds against the target E. coli DNA gyrase to determine their binding affinity within the enzyme’s active site. Moreover, ADME evaluations of these compounds predicted their high oral bioavailability and good GI absorption.
In sight on olive oil maceration and supercritical CO2 in extracting rosemary essential oil
The flavor, nutritional, and medicinal value of rosemary are well known. Hydrodistilled (HD) essential oil was prepared in the present study as a standard. Olive oil maceration (OM) and supercritical carbon dioxide (SC-CO 2 ) technology were separately applied to extract the essential oil of rosemary. The three obtained products, HD, OM, and SC-CO 2 , were compared concerning their main constituents using GC‒MS. Their antimicrobial properties were evaluated against eight microbes by the disc diffusion assay. Interestingly, both 1,8-cineol and camphor were the major compounds in the three oils. α-Pinene was also detected in large amounts in both HD and OM. Additionally, borneol was the third major component in SC-CO 2 . The antimicrobial results revealed differential effects against six microbes. However, HD oil also exhibited antifungal activity. Maceration is a green extraction procedure that is easy to perform in households, and attention must be paid to olive oil maceration as a complementary medicine that originated in pharaohs.
Novel Pyridothienopyrimidine Derivatives: Design, Synthesis and Biological Evaluation as Antimicrobial and Anticancer Agents
The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set of pyridothienopyrimidine derivatives 2a,b–9a,b was synthesized via cyclization reactions of 3-amino-thieno[2,3-b]pyridine-2-carboxamides 1a,b with different reagents. All new compounds were evaluated against five bacterial and five fungal strains. Many of the target compounds showed significant antimicrobial activity. In addition, the new derivatives were further subjected to cytotoxicity evaluation against HepG-2 and MCF-7 cancer cell lines. The most potent cytotoxic candidates (3a, 4a, 5a, 6b, 8b and 9b) were examined as EGFR kinase inhibitors. Molecular docking study was also performed to explore the binding modes of these derivatives at the active site of EGFR-PK. Compounds 3a, 5a and 9b displayed broad spectrum antimicrobial activity with MIC ranges of 4–16 µg/mL and potent cytotoxic activity with IC50 ranges of 1.17–2.79 µM. In addition, they provided suppressing activity against EGFR with IC50 ranges of 7.27–17.29 nM, higher than that of erlotinib, IC50 = 27.01 nM.
Synthesis and Biological Evaluation of New Pyridothienopyrimidine Derivatives as Antibacterial Agents and Escherichia coli Topoisomerase II Inhibitors
The growing resistance of bacteria to many antibiotics that have been in use for several decades has generated the need to discover new antibacterial agents with structural features qualifying them to overcome the resistance mechanisms. Thus, novel pyridothienopyrimidine derivatives (2a,b–a,b) were synthesized by a series of various reactions, starting with 3-aminothieno[2,3-b]pyridine-2-carboxamides (1a,b). Condensation of compounds 1a,b with cyclohexanone gave 1’H-spiro[cyclohexane-1,2’-pyrido[3’,2’:4,5]thieno[3,2-d]pyrimidin]-4’(3’H)-ones (2a,b), which in turn were utilized to afford the target 4-substituted derivatives (3a,b–8a,b). In vitro antibacterial activity evaluations of all the new compounds (2a,b–8a,b) were performed against six strains of Gram-negative and Gram-positive bacteria. The target compounds showed significant antibacterial activity, especially against Gram-negative strains. Moreover, the compounds (2a,b; 3a,b; 4a,b; and 5a,b) that exhibited potent activity against Escherichia coli were selected to screen their inhibitory activity against Escherichia coli topoisomerase II (DNA gyrase and topoisomerase IV) enzymes. Compounds 4a and 4b showed potent dual inhibition of the two enzymes with IC50 values of 3.44 µΜ and 5.77 µΜ against DNA gyrase and 14.46 µΜ and 14.89 µΜ against topoisomerase IV, respectively. In addition, docking studies were carried out to give insight into the binding mode of the tested compounds within the E. coli DNA gyrase B active site compared with novobiocin.
Cell immobilization for enhanced milk clotting enzyme production from Bacillus amyloliquefacien and cheese quality
Background Milk clotting enzymes, essential for milk coagulation in cheese production, are obtained from the stomach of young ruminants, an expensive and limited source. This study was accomplished by finding a suitable alternative. Bacterial isolates recovered from honey were screened for milk clotting enzyme activity. and further, by immobilization of the microorganisms to enhance stability and facilitate their repeated use. Result The most effective enzyme was produced by a microbe identified as Bacillus amyloliquefaciens based on 16 S rRNA sequencing. The cells were encapsulated in Ca 2+ alginate beads. These beads retained complete enzyme production after being used five times. Glucose and Soybean were selected as the most favorable carbon and nitrogen sources, respectively. The optimum temperature for activity was 35 ℃ for both free and immobilized cells but as the temperature was increased to 55 °C and above, the encapsulated form retained more activity than the free cells. The pH optimum shifted from 6.5 to 7 for the free cells to 7–7.5 for the immobilized cells. The immobilization process decreased the activation energy for enzyme production and activity, prolonged the enzyme half-life, and increased the deactivation energy. Enzyme produced by immobilized cells generated a more compact cheese. Conclusions The finding of this study was to identify a less expensive source of milk-clotting enzymes and confirm the success of cell immobilization in improving cell rigidity and stability. Also, immobilization of this B. amyloliquefaciens strain offers an enzyme source of value for industrial production of cheese.
In sight on olive oil maceration and supercritical CO 2 in extracting rosemary essential oil
The flavor, nutritional, and medicinal value of rosemary are well known. Hydrodistilled (HD) essential oil was prepared in the present study as a standard. Olive oil maceration (OM) and supercritical carbon dioxide (SC-CO ) technology were separately applied to extract the essential oil of rosemary. The three obtained products, HD, OM, and SC-CO , were compared concerning their main constituents using GC‒MS. Their antimicrobial properties were evaluated against eight microbes by the disc diffusion assay. Interestingly, both 1,8-cineol and camphor were the major compounds in the three oils. α-Pinene was also detected in large amounts in both HD and OM. Additionally, borneol was the third major component in SC-CO . The antimicrobial results revealed differential effects against six microbes. However, HD oil also exhibited antifungal activity. Maceration is a green extraction procedure that is easy to perform in households, and attention must be paid to olive oil maceration as a complementary medicine that originated in pharaohs.
A hybrid mesoporous composite of SnO2 and MgO for adsorption and photocatalytic degradation of anionic dye from a real industrial effluent water
Water pollution by synthetic anionic dyes is one of the most critical ecological concerns and challenges. Therefore, there is an urgent need to find an efficient adsorbent and photocatalyst for dye removal. In the present study, we aimed to fabricate a hybrid mesoporous composite of spongy sphere-like SnO 2 and three-dimensional (3D) cubic-like MgO (SnO 2 /MgO) as a promising adsorbent/photocatalyst to remove the anionic sunset yellow (SSY) dye from real wastewater at neutral pH conditions. The as-synthesized SnO 2 and MgO composite was investigated using XRD, SEM, EDX, TEM, XPS, BET, and zeta potential. The experimental study of the SSY removal using SnO 2 /MgO composite was performed at different conditions, such as pH, stirring time, dose, and temperature. More than 99% of 10 mg/L SSY was effectively adsorbed from aqueous solution using 40 mg of SnO 2 /MgO composite at pH 7 and a stirring time of 60 min. The SSY adsorption behavior was well fitted by pseudo-second order and the Langmuir model, indicating that the SSY was chemisorbed to the composite-active sites as a monolayer. On the other hand, photocatalytic degradation process exhibited better results in terms of speed of removal and used quantity of photocatalyst, where 20 mg of SnO 2 /MgO composite can be used to remove > 99% of SSY dye within 30 min. Mechanism of SSY adsorption and photocatalytic degradation was discussed. In addition, elution experiments demonstrated that the SnO 2 /MgO composite as an SSY adsorbent could be reused for nine cycles without considerable reduction in the SSY adsorption efficiency. Therefore, this work exhibited that the mesoporous SnO 2 /MgO composite can be considered an effective adsorbent/photocatalyst to remove SSY dye from real industrial effluent water at neutral pH conditions.
A robust framework for evaluating green mines towards sustainable development
The development of green mines is essential for promoting sustainability in the mining sector due to the significant ecological impacts of resource extraction. This study proposes a novel hybrid multi-criteria decision-making (MCDM) framework that integrates Spherical Fuzzy Sets (SFSs) with SWOT analysis, the CRITIC method, and Grey Relational Analysis (GRA). The framework introduces several innovations: it applies SFS-based MCDM for the first time to green mine evaluation in Egypt, structures 37 sustainability-related criteria under SWOT dimensions, and employs SF-CRITIC for objective weighting without subjective comparisons. The model is applied to assess 20 gold mines, where the SF-GRA method is used to rank alternatives based on proximity to an ideal solution. The results show that GME20 consistently ranks highest, while GME5 ranks lowest. A sensitivity analysis is conducted by varying the Grey relational coefficient and simulating 37 weight scenarios, demonstrating stable rankings and strong model resilience. Comparative analysis against ten SFS-based MCDM methods confirms the consistency of results, with Spearman correlation coefficients exceeding 0.77. In addition to its methodological novelty, the framework supports interpretable decision outcomes by identifying key sustainability drivers such as renewable energy adoption and land reclamation. This contributes actionable insights for policymakers and stakeholders, enabling informed green investment and regulatory decisions. The study offers a transparent, reproducible, and scalable tool for sustainability evaluation in resource-intensive industries. The proposed model introduces a structured integration of SWOT-based criteria classification, objective weight computation via SF-CRITIC, and robust alternative ranking using SF-GRA. Furthermore, it contributes uniquely by applying the methodology to the underexplored context of green mine evaluation in Egypt. These distinctions articulate the methodological and application-based novelties of the proposed framework.
Evaluation of nitazoxanide treatment following triclabendazole failure in an outbreak of human fascioliasis in Upper Egypt
Fascioliasis is a neglected zoonosis with major public health implications in humans. Although triclabendazole (TCBZ) is the drug of choice, there are records of TCBZ failure worldwide. TCBZ-resistant fascioliasis is treated with alternative approved drugs including nitazoxanide (NTZ), with varying levels of efficacy. Data on NTZ efficacy after TCBZ failure in Egypt is scarce. This study evaluated the efficacy of NTZ in cases of TCBZ failure during an outbreak of fascioliasis in Assiut governorate of Upper Egypt. This prospective study included 67 patients from the outpatient clinic in Manfalout locality of Assiut governorate with clinical manifestations of acute fascioliasis. These included high eosinophilia (> 6% eosinophils in peripheral blood), positive anti-Fasciola antibodies, and hepatic focal lesions (HFL) or ascites on abdominal ultrasound or computed tomography. All patients initially received TCBZ at recommended doses. Patients were followed up after 1 month to assess response. According to the responses, patients were categorized as non-responders and responders. The non-responders received a trial of NTZ and were re-assessed for response based on clinical manifestations, eosinophil count, and abdominal ultrasound. Patients not responding to NTZ received additional doses of TCBZ. One month after initial TCBZ treatment, 37 patients responded well to TCBZ, while 30 patients failed to respond with persistence of fever, abdominal pain, high eosinophilia, and HFL. Most non-responders were male (56.7%); females predominated among TCBZ responders (62.2%). The mean age of the non-responders was relatively lower, at 20.57 ± 14.47 years (p = 0.004). Following NTZ therapy, HFL disappeared in 9/30 (30%) patients and eosinophil counts normalized in only 2 (6.7%) patients, indicating an overall efficacy of 36.6%. The remaining cases received additional doses of TCBZ with complete clinical, pathological, and radiological resolution. Nitazoxanide was partially effective in TCBZ failure in acute human fascioliasis in Upper Egypt. Further studies with larger samples are highly encouraged and further research is urgently needed to find new therapeutic alternatives to TCBZ.