New 1,3,4-oxadiazole-chalcone/benzimidazole hybrids as potent antiproliferative agents.

A series of new 1,3,4-oxadiazole-chalcone/benzimidazole hybrids 9a-o and 10a-k were designed and synthesized as potential antiproliferative agents. Hybrids 9a-o exhibited remarkable antiproliferative activities on different NCI-60 cell lines in a single-dose assay. The antiproliferative activities of the newly synthesized compounds were evaluated against a panel of four human cancer cell lines (A-549, MCF-7, Panc-1, and HT-29).

The Pattern of Antimicrobial Prescription at a Tertiary Health Center in Egypt: A Point Survey and Implications.

Background: The misuse of antimicrobials has major consequences, particularly antimicrobial resistance (AMR) and antimicrobials' related adverse effects. So, the WHO proposed antimicrobial surveillance to improve antimicrobials use. This point prevalence survey (PPS) was conducted to illustrate the prevalence of antimicrobial use at Mansoura University hospitals (MUH), Egypt.

Anti-prostate cancer metabolites from the soil-derived .

Prostate cancer (PCa) ranks as one of the most commonly diagnosed malignancies worldwide. Toxicity, lack of clinical efficacy, and development of resistance phenotypes are the main challenges in the control of prostate malignancies. Notably, castration-resistance prostate cancer (CRPCa) is a highly aggressive and metastatic phenotype of the disease with a poor prognosis and very limited therapeutic options.

Human MHC class I molecule, HLA-A2.1, mediates activation of CD8 T cell IFN-γ production and the T cell-dependent protection against reactivation of cerebral infection.

To examine whether the HLA-A2.1, one of the most common MHC class I molecules in humans, activates the protective immunity against reactivation of cerebral infection with , HLA-A2.1-transgenic and wild-type (WT) mice were infected and treated with sulfadiazine to establish chronic infection in their brains.

Synthesis and Identification of New ,-Disubstituted Thiourea, and Thiazolidinone Scaffolds Based on Quinolone Moiety as Urease Inhibitor.

Synthesis of thiazolidinone based on quinolone moiety was established starting from 4-hydroxyquinol-2-ones. The strategy started with the reaction of ethyl bromoacetate with 4-hydroxyquinoline to give the corresponding ethyl oxoquinolinyl acetates, which reacted with hydrazine hydrate to afford the hydrazide derivatives. Subsequently, hydrazides reacted with isothiocyanate derivatives to give the corresponding ,-disubstituted thioureas.

Benzimidazole Bearing Thiosemicarbazone Derivatives Act as Potent α-Amylase and α-Glucosidase Inhibitors; Synthesis, Bioactivity Screening and Molecular Docking Study.

Diabetes mellitus is one of the most chronic metabolic diseases. In the past few years, our research group has synthesized and evaluated libraries of heterocyclic analogs against α-glucosidase and α-amylase enzymes and found encouraging results. The current study comprises the evaluation of benzimidazole-bearing thiosemicarbazone as antidiabetic agents.

Epstein-Barr virus, interleukin-10 and multiple sclerosis: A ménage à trois.

Multiple Sclerosis (MS) is an autoimmune disease that is characterized by inflammation and demyelination of nerve cells. There is strong evidence that Epstein-Barr virus (EBV), a human herpesvirus infecting B cells, greatly increases the risk of subsequent MS. Intriguingly, EBV not only induces human interleukin-10 but also encodes a homologue of this molecule, which is a key anti-inflammatory cytokine of the immune system.

GC-MS Profiling, Anti-, and Anti-Inflammatory Activities of Three Apiaceous Fruits' Essential Oils.

Eradication of is a challenge due to rising antibiotic resistance and GIT-related disorders. , and are fruits belonging to the Apiaceae family. Their essential oils were extracted, analyzed using GC-MS, tested for anti- activity by a micro-well dilution technique, identified for potential anti- inhibitors by an in-silico study, and investigated for anti-inflammatory activity using a COX-2 inhibition assay.

Recent advances in the treatment of childhood asthma: a clinical pharmacology perspective.

Introduction: Childhood asthma is a complex heterogenous inflammatory disease that can pose a large burden on patients and their caregivers. There is a strong need to adapt asthma treatment to the individual patient taking into account underlying inflammatory profiles, moving from a 'one size fits all' approach toward a much-needed personalized approach.

Areas Covered: This review article aims to provide an overview of recent advances in the management and treatment of pediatric asthma, including novel insights on the molecular heterogeneity of childhood asthma, the emergence of biologicals to treat severe asthma, and innovative e-health and home monitoring techniques to make asthma management more convenient and accessible.

Determining the Site of Upper Airway Narrowing in Snorers Using a Noninvasive Technique.

Background In this study, we aimed to determine the site of obstruction if surgical treatment is considered. Flexible nasopharyngoscopy is an invasive procedure currently used for the assessment of snoring and the level of obstruction. Here, we examine the role of Somnoscreen™ plus, a noninvasive cardiorespiratory polysomnographic device, in identifying the site of obstruction in patients presenting with snoring.

Selective protein kinase C inhibition switches time-dependent glucose cardiotoxicity to cardioprotection.

Hyperglycaemia at the time of myocardial infarction has an adverse effect on prognosis irrespective of a prior diagnosis of diabetes, suggesting glucose is the damaging factor. In models of ischaemia, we demonstrated that deleterious effects of acutely elevated glucose are PKCα/β-dependent, and providing PKCα/β are inhibited, elevated glucose confers cardioprotection. Short pre-treatments with high glucose were used to investigate time-dependent glucose cardiotoxicity, with PKCα/β inhibition investigated as a potential mechanism to reverse the toxicity.

New potent ciprofloxacin-uracil conjugates as DNA gyrase and topoisomerase IV inhibitors against methicillin-resistant Staphylococcus aureus.

A series of ciprofloxacin-uracil conjugates 5a-t were synthesized and identified by H NMR, C NMR, mass spectroscopy and elemental analyses. The antibacterial results revealed that the new derivatives exhibited better activity against Gram-positive than the Gram-negative strains; most of the target compounds exhibited good activities against S. aureus ATCC 6538.

Multipotent Cholinesterase Inhibitors for the Treatment of Alzheimer's Disease: Synthesis, Biological Analysis and Molecular Docking Study of Benzimidazole-Based Thiazole Derivatives.

Twenty-four analogues of benzimidazole-based thiazoles (-) were synthesized and assessed for their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory potential. All analogues were found to exhibit good inhibitory potential against cholinesterase enzymes, having IC values in the ranges of 0.10 ± 0.

Novel diaryl ether derivatives as InhA inhibitors: Design, synthesis and antimycobacterial activity.

A new series of triclosan (TCL)-mimicking diaryl ether derivatives 7-25 were synthesized and evaluated as inhibitors of enoyl acyl carrier protein reductase InhA enzyme. In addition, these derivatives were screened as inhibitors of drug-susceptible (DS), multidrug-resistant (MDR), and extensive drug-resistant (XDR) Mycobacterium tuberculosis (MTB) strains. Most compounds exihibted superior anti-TB activities and improved ClogP compared to TCL as a standard drug.

Accuracy of digital auricular impression using intraoral scanner versus conventional impression technique for ear rehabilitation: A controlled clinical trial.

Purpose: This research aims to compare the accuracy of different auricular impression techniques used to produce either a mirror image of the unaffected ear or a surgical stent and template for auricular rehabilitation. The research compares two digital ear impression techniques using an Intra-Oral digital Scanner (IOS) (with /without markers) versus a traditional technique using hydrocolloid impression materials.

Material And Methods: Eight participants were selected with intact right ears.

Genomic analyses of the Linum distyly supergene reveal convergent evolution at the molecular level.

Supergenes govern multi-trait-balanced polymorphisms in a wide range of systems; however, our understanding of their origins and evolution remains incomplete. The reciprocal placement of stigmas and anthers in pin and thrum floral morphs of distylous species constitutes an iconic example of a balanced polymorphism governed by a supergene, the distyly S-locus. Recent studies have shown that the Primula and Turnera distyly supergenes are both hemizygous in thrums, but it remains unknown whether hemizygosity is pervasive among distyly S-loci.

Silica-Coated Magnetic Nanoparticles for Vancomycin Conjugation.

Drug resistance is a global health challenge with thousands of deaths annually caused by bacterial multidrug resistance (MDR). Efforts to develop new antibacterial molecules do not meet the mounting needs imposed by the evolution of MDR. An alternative approach to overcome this challenge is developing targeted formulations that can enhance the therapeutic efficiency and limit side effects.

Synthesis, Molecular Docking, c-Met Inhibitions of 2,2,2-Trichloroethylidene- cyclohexane-1, 3-dione Derivatives Together with their Application as Target SARS-CoV-2 main Protease (Mpro) and as Potential anti-COVID-19.

Background: The lack of anti-COVID-19 treatment to date warrants urgent research into potential therapeutic targets. Virtual drug screening techniques enable the identification of novel compounds that target the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Main Protease (M).

Objective: The binding of the halogenated compounds to M may inhibit the replication and transcription of SARS-CoV-2 and, ultimately, stop the viral life cycle.

MicroCT evaluation for CAD/CAM occlusal veneer fit using two materials and three cement space settings.

This study was aimed to evaluate the fit of occlusal veneer restoration for two CAD/CAM materials with different cement space settings, using microCT scans. Sixty resin dies were made and divided into two groups (n=30) according to the materials, (I): Hybrid all-ceramic, and (II): zirconia-reinforced lithium silicate glass-ceramic. Each group was subdivided into three subgroups (n=10) according to the cement space parameters (30, 40, and 50 µm).

Enhanced In Vivo Wound Healing Efficacy of a Novel Hydrogel Loaded with Copper (II) Schiff Base Quinoline Complex (CuSQ) Solid Lipid Nanoparticles.

Wound dressings created using nanotechnology are known as suitable substrates to speed up the healing of both acute and chronic wounds. Therapeutic substances can be delivered using these materials. In this study, a hydrogel loaded with Cu (II) Schiff base 8-hydroxy quinoline complex (CuSQ) solid lipid nanoparticles (SLN) was formulated to investigate its wound healing potential in an excision wound healing model in rats.

High Thermoelectric Power Generation by SWCNT/PPy Core Shell Nanocomposites.

Polypyrrole (PPy) is a conducting polymer with attractive thermoelectric (TE) properties. It is simple to fabricate and modify its morphology for enhanced electrical conductivity. However, such improvement is still limited to considerably enhancing TE performance.

Comparative effect of transforaminal injection of Magnesium sulphate versus Ozone on oxidative stress biomarkers in lumbar disc related radicular pain.

Background: We aimed to investigate the effect of transforaminal injection of Magnesium sulphate versus Ozone on pain intensity, functional disability and the oxidative stress biomarkers; superoxide dismutase (SOD) and Glutathione (GSH) in patients with lumbar disc prolapse.

Methods: This randomized controlled trial was conducted on 135 patients having symptomatic lumbar disc prolapse, received either transforaminal injection of Magnesium sulphate with steroids, Ozone with steroids, or steroids alone. Assessment of pain severity and functional disability were done before intervention, 2 weeks, 1, 3, and 6 months after intervention.

Determination of Therapeutic and Safety Effects of Extract in Induced Inflammation in Rats.

Background: is a facultative plant with many medicinal applications. This study examined the anti-inflammatory activity of () in an arthritis animal model.

Materials And Methods: Seventy-Six Wistar Albino rats of either sex randomly divided into six groups (12/each).