Insight on novel sulfamoylphenyl pyrazole derivatives as anticancer carbonic anhydrase inhibitors.

As another part continue for our previous study, variable substituted pyrazoles bearing sulfamoylphenyl moiety were synthesized and screened against two cancer related human carbonic anhydrase (hCA) isoforms and acetazolamide (AAZ) used as a reference standard. Some compounds as 4e and 6c manifested a promising inhibitory activity against both isoforms (K = 0.072, 0.

Discovery of pyrazole-based analogs as CDK2 inhibitors with apoptotic-inducing activity: design, synthesis and molecular dynamics study.

The discovery of novel CDK2 inhibitors is crucial for developing targeted anticancer therapies. Thus, in this study, we aimed to design, synthesize, and evaluate a series of novel pyrazole derivatives (2a-g, 7a-d, 8a and b, 9, and 10) for their potential as CDK2/cyclin A2 enzyme inhibitors. The newly synthesized compounds were screened at 50 μM for CDK2 inhibition, followed by IC profiling of the most promising candidates.

Energy-conversion efficiency for producing oxy-hydrogen gas using a simple generator based on water electrolysis.

Producing hydrogen efficiently through water electrolysis could greatly reduce fossil fuel consumption. As well as this renewable energy source will also help combat global warming and boost economic investment opportunities. This paper studied some factors affecting the performance of oxy-hydrogen/hydroxy (HHO) gas generator, such as applied voltage (from 10.

Brain state-dependent repetitive transcranial magnetic stimulation for motor stroke rehabilitation: a proof of concept randomized controlled trial.

Background: In healthy subjects, repetitive transcranial magnetic stimulation (rTMS) targeting the primary motor cortex (M1) demonstrated plasticity effects contingent on electroencephalography (EEG)-derived excitability states, defined by the phase of the ongoing sensorimotor μ-oscillation. The therapeutic potential of brain state-dependent rTMS in the rehabilitation of upper limb motor impairment post-stroke remains unexplored.

Objective: Proof-of-concept trial to assess the efficacy of rTMS, synchronized to the sensorimotor μ-oscillation, in improving motor impairment and reducing upper-limb spasticity in stroke patients.

Metal complexes featuring a quinazoline schiff base ligand and glycine: synthesis, characterization, DFT and molecular docking analyses revealing their potent antibacterial, anti-helicobacter pylori, and Anti-COVID-19 activities.

Mixed ligand complexes of manganese(II), cobalt(II), copper(II), and cadmium(II)with an innovative Schiff base ligand denoted as (L), 4-(2-((1E,2E)-1-(2-(p-tolyl)hydrazineylidene)propan-2-ylidene)hydrazineyl), served as the principal ligand, while glycine (L2) was employed as secondary ligand were successfully effectively characterized through a comprehensive set of analyses, including Elemental analysis, UV-Visible, FT-IR, Mass spectra, and conductometric measurements. Density functional theory (DFT) computations were executed to discern the enduring electronic arrangement, the energy gap, dipole moment and chemical hardness of the hybrid ligand assemblies. The proposed geometry for the complexes is a distorted octahedral structure.

Bitter tastants relax the mouse gallbladder smooth muscle independent of signaling through tuft cells and bitter taste receptors.

Disorders of gallbladder motility can lead to serious pathology. Bitter tastants acting upon bitter taste receptors (TAS2R family) have been proposed as a novel class of smooth muscle relaxants to combat excessive contraction in the airways and other organs. To explore whether this might also emerge as an option for gallbladder diseases, we here tested bitter tastants for relaxant properties and profiled Tas2r expression in the mouse gallbladder.

Insight on Some Newly Synthesized Trisubstituted Imidazolinones as VEGFR-2 Inhibitors.

Two series of ten new 1,2,4-trisubstituted imidazolin-5-ones were synthesized and screened against MCF-7 breast cancer and A549 lung cancer cell lines to test their potential in vitro anticancer activity. The results revealed preferential activity of the tested compounds toward MCF-7 cell lines compared to A549 cell lines. The most promising ten compounds (, , , , , , , , , and ) were subjected to VEGFR-2 enzyme inhibitory activity testing to further explore their mechanism of action.

How did the use of the social marketing approach in Egyptian communities succeed in improving breastfeeding practices and infants' growth?

Introduction: Improving breastfeeding practices does not always link to interventions relying only on improving nutrition awareness and education but needs cultural and behavioral insights .

Aim: This study aimed to evaluate the changes in core breastfeeding indicators as a result of the use of social marketing (SM) approach for improving breastfeeding practices of Egyptian women and the physical growth of infants aged 6 to 12 months. The core breastfeeding indicators were: Early initiation of breastfeeding within one hour of birth, Predominant and exclusive breastfeeding to 6 months (EBF), Bottle feeding with formula, continued breastfeeding to 1 and 2 years, and responsiveness to cues of hunger and satiety.

Utility of sulfachloropyridazine in the synthesis of novel anticancer agents as antiangiogenic and apoptotic inducers.

In a search for new anticancer agents with better activity and selectivity, the present work described the synthesis of several new series of sulfachloropyridazine hybrids with thiocarbamates 3a-e, thioureids 4a-h, 5a-e and 4-substituted sulfachloropyridazines 6a, b, 7a, b and 8. The synthesized compounds were screened in vitro against a panel of 60 cancer cell lines in one dose assay. The most potent derivatives 3a, 3c, 4c, 4d, 5e, 7a and 7b were tested for their antiangiogenic activity by measuring their ability to inhibit VEGFR-2.

Molecular docking approach for the design and synthesis of new pyrazolopyrimidine analogs of roscovitine as potential CDK2 inhibitors endowed with pronounced anticancer activity.

Cyclin-dependent kinase 2 (CDK2) is a vital protein for controlling cell cycle progression that is critically associated with various malignancies and its inhibition could offer a convenient therapeutic approach in designing anticancer remedies. Consequently, this study aimed to design and synthesize new CDK2 inhibitors featuring roscovitine as a template model. The purine ring of roscovitine was bioisosterically replaced with the pyrazolo[3,4-d]pyrimidine scaffold, in addition to some modifications in the side chains.

Design, synthesis, and biological evaluation of dinaciclib and CAN508 hybrids as CDK inhibitors.

The scaffolds of two known CDK inhibitors (CAN508 and dinaciclib) were the starting point for synthesizing two series of pyarazolo[1,5-a]pyrimidines to obtain potent inhibitors with proper selectivity. The study presented four promising compounds; 10d, 10e, 16a, and 16c based on cytotoxic studies. Compound 16a revealed superior activity in the preliminary anticancer screening with GI % = 79.

A hybrid brain-muscle-machine interface for stroke rehabilitation: Usability and functionality validation in a 2-week intensive intervention.

The primary constraint of non-invasive brain-machine interfaces (BMIs) in stroke rehabilitation lies in the poor spatial resolution of motor intention related neural activity capture. To address this limitation, hybrid brain-muscle-machine interfaces (hBMIs) have been suggested as superior alternatives. These hybrid interfaces incorporate supplementary input data from muscle signals to enhance the accuracy, smoothness and dexterity of rehabilitation device control.

Esophageal cancer: a twenty-four-year experience at a tertiary care center with an evaluation of the prognostic significance of the neutrophil-lymphocyte ratio.

Background: A high neutrophil-lymphocyte ratio (NLR) may be associated with worse survival in esophageal cancer (EC). Our aims were to describe the demographic and clinical data of EC in a tertiary referral center in Lebanon and to determine the prognostic value of NLR.

Methods: A retrospective cohort study based on chart review of patients diagnosed with EC was conducted at the American University of Beirut Medical Center (AUBMC).

Added value of 3D THRIVE (T1-weighted high-resolution isotropic volume examination) MRI pulse sequence in the detection of bony erosions of sacroiliac joints in patients of spondyloarthritis.

Purpose: Early depiction of bony erosions in sacroiliac (SI) joints increases the diagnostic accuracy of spondyloarthritis. The new 3D magnetic resonance imaging (MRI) sequence THRIVE (T1-weighted high-resolution isotropic volume examination) can depict cartilage erosions in sacroiliac joints. The aim of the study was to compare the diagnostic capacity of the new MRI sequence 3D THRIVE (T1-weighted high-resolution isotropic volume examination) with the routinely used T1 TSE pulse sequence in the depiction of structural erosions in sacroiliac joints by using MRI sequence zero echo time (zero ET) as a reference standard.

Removal of chromium from tannery industry wastewater using iron-based electrocoagulation process: experimental; kinetics; isotherm and economical studies.

Chromium is a hazardous compound from industrial processes, known for its toxicity, mutagenicity, teratogenicity, and carcinogenicity. Chemical methods are efficient but cost-effective alternatives with reduced sludge are sought. Electro-coagulation, utilizing low-cost iron plate electrodes, was explored for factual tannery wastewater treatment in this manuscript.

Testing spasticity mechanisms in chronic stroke before and after intervention with contralesional motor cortex 1 Hz rTMS and physiotherapy.

Background: Previous studies showed that repetitive transcranial magnetic stimulation (rTMS) reduces spasticity after stroke. However, clinical assessments like the modified Ashworth scale, cannot discriminate stretch reflex-mediated stiffness (spasticity) from passive stiffness components of resistance to muscle stretch. The mechanisms through which rTMS might influence spasticity are also not understood.

Effect of blood flow restriction as a stand-alone treatment on muscle strength, dynamic balance, and physical function in female patients with chronic ankle instability.

Background: Blood Flow Restriction (BFR) training has gained popularity as a novel training strategy in athletes and rehabilitation settings in recent years.

Objective: To investigate whether BFR as a stand-alone treatment would affect muscle strength, dynamic balance, and physical function in female patients with chronic ankle instability (CAI).

Methods: Thirty-nine patients with CAI were randomly allocated into 1 of 3 groups: BFR as a stand-alone (BFR) group, BFR with rehabilitation (BFR+R) group, and rehabilitation (R) group.

Challenges of neural interfaces for stroke motor rehabilitation.

More than 85% of stroke survivors suffer from different degrees of disability for the rest of their lives. They will require support that can vary from occasional to full time assistance. These conditions are also associated to an enormous economic impact for their families and health care systems.

Exploring novel anticancer pyrazole benzenesulfonamides featuring tail approach strategy as carbonic anhydrase inhibitors.

This study aimed to design potent carbonic anhydrase inhibitors (CAIs) based on pyrazole benzenesulfonamide core. Nine series of substituted pyrazole benzenesulfonamide compounds were synthesized with variable groups like sulphamoyl group as in compounds 4a-e, its bioisosteric carboxylic acid as in compounds 5a-e and 8e, ethyl carboxylate ester as in compounds 6a-e and 9a-e, which were designed as potential prodrugs, isothiazole ring as in compound 7, hydrazide derivative 10e, hydroxamic acid derivatives 11a-e and semicarbazide derivatives 12a-c,e. All the synthesized compounds were investigated for their carbonic anhydrase (CA) inhibitory activity against two human CA isoforms hCA IX and hCA XII and compared to acetazolamide (AAZ).

Measuring resistance to externally induced movement of the wrist joint in chronic stroke patients using an objective hand-held dynamometer.

Objective: We evaluated the resistance to externally induced wrist extension in chronic stroke patients. We aimed to objectively measure and distinguish passive (muscle and soft tissue stiffness) and active (spasticity and spastic dystonia) components of the resistance.

Methods: We used a hand-held dynamometer, which measures torque, joint movement and electromyography (EMG) simultaneously, to assess the resistance to externally induced wrist extension.

Versatility of Local Fasciocutaneous Island Flaps for Resurfacing Soft Tissue Defects Overlying the Achilles Tendon.

Background: Reconstruction of soft tissue defects overlying the Achilles tendon has always been a challenge. Various modalities of reconstruction have been described to resurface such defects. We aimed to assess the functional and cosmetic outcomes of all patients who had undergone reconstruction of small and medium sized soft tissue defects of the Achilles region using local fasciocutaneous island flaps.

Assessment of macronutrients dietary intake, central adiposity among pre- and postmenopausal Egyptian women with benign and malignant breast tumors.

Background: Breast cancer (BC) is the second most frequent cancer in women and the second most common cancer worldwide. Lifestyle factors, like body weight, physical activity and diet, may be accompanying with higher BC risk.

Aim: The assessment of macronutrients dietary intake; protein, fat, carbohydrates and their components of amino, fatty acids, and central obesity/adiposity among pre- and postmenopausal Egyptian women with benign and malignant breast tumors.

Effect of hydrophobic extension of aryl enaminones and pyrazole-linked compounds combined with sulphonamide, sulfaguanidine, or carboxylic acid functionalities on carbonic anhydrase inhibitory potency and selectivity.

Design and synthesis of three novel series of aryl enaminones (- and -) and pyrazole () linked compounds with sulphonamides, sulfaguanidine, or carboxylic acid functionalities were reported as carbonic anhydrase inhibitors (CAIs) using the "tail approach" strategy in their design to achieve the most variable amino acids in the middle/outer rims of the hCAs active site. The synthesised compounds were assessed for their inhibitory activity against the following human (h) isoforms, hCA I, II, IX, and XII using stopped-flow CO hydrase assay. Enaminone sulphonamide derivatives (-) potently inhibited the target tumour-associated isoforms hCA IX and hCA XII (KIs 26.

A misdiagnosed case of a 150-cm umbilical cord coiled twice around the fetal neck with a true cord knot: A rare Syrian case report.

The normal umbilical cord is a crucial component during pregnancy, but sometimes it could become compromised due to some abnormalities such as excessive long umbilical cord, and though they usually end up with a healthy baby, they may lead to severe consequences. Excessive long umbilical cords are found in 4% of pregnancies and represent a risk factor for nuchal cords and true knots. We report a case of a 37-year-old Syrian pregnant woman who presented to the hospital at 37 weeks of gestation asking for a C-section for a fear of ambiguous ultrasound findings that have been interpreted as fetal malformation.