What Is the Most Optimal Bearing Surface for Minimizing Instability After Revision Total Hip Arthroplasty?

Based on the results of our meta-analysis, dual mobility implants appear to have the most efficacy in preventing instability following revision total hip arthroplasty. Notwithstanding, given the relatively small sample sizes of the included studies, in conjunction with heterogeneity in study design, it is important to recognize that further large randomized controlled trials are necessary to determine the optimal bearing surface to reduce the risk of instability after revision total hip arthroplasty.

Assessment of the implementation of risk minimization measures for bosentan: a retrospective study.

Background: Bosentan is associated with adverse hepatic effects. To minimize such risk, regulators implemented risk minimization measures (RMMs), including testing for liver injury biomarkers (alanine and aspartate transaminase and bilirubin) prior to therapy initiation and monthly throughout therapy. This study aimed to examine the adherence to hepatic monitoring requirements.

Covalent small-molecule inhibitors of SARS-CoV-2 Mpro: Insights into their design, classification, biological activity, and binding interactions.

Since 2020, many compounds have been investigated for their potential use in the treatment of SARS-CoV-2 infection. Among these agents, a huge number of natural products and FDA-approved drugs have been evaluated as potential therapeutics for SARS-CoV-2 using virtual screening and docking studies. However, the identification of the molecular targets involved in viral replication led to the development of rationally designed anti-SARS-CoV-2 agents.

Assessment of Monitoring and Management Practices of Antipsychotic-Induced Hyperprolactinemia at a Medical City in Riyadh, Saudi Arabia: A Retrospective Cohort Study.

Background: Hyperprolactinemia is a commonly underestimated adverse effect of antipsychotic medications. There are still no consensus guidelines for the optimal monitoring and treatment strategies.

Objective: The aim of the study was to assess the monitoring and treatment practices of antipsychotic-induced hyperprolactinemia, in addition to the prevalence and risk factors associated with it.

Does sequential examination under anaesthesia provide a reliable method to determine a management plan for unstable lateral compression pelvic ring injuries? a prospective study.

Purpose: To assess the reliability of sequential examination under anaesthesia (EUA) to determine pelvic instability and to evaluate radiological and functional outcomes in unstable lateral compression (LC) injuries.

Methods: A prospective case series study was conducted from 2020 to 2022 at a university hospital on 43 cases with LC injuries that met the inclusion criteria. Sequential EUA was carried out in three steps.

New Sulfamethoxazole Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors: Design, Synthesis, Cytotoxic Activity and Molecular Modeling.

In this study new sulphamethoxazole derivatives (, , and ) were designed and synthesized and their structures were fully characterized and validated using NMR, mass, and IR spectroscopy, as well as elemental analyses. All new derivatives () were assayed against human carbonic anhydrase (hCAs IX and XII) for their inhibitory activities. hCAs IX and XII were chosen due to the fact that CAIX expression is recognized as a hypoxia marker with a poor prognosis in breast cancer.

A Comprehensive Overview of Globally Approved JAK Inhibitors.

Janus kinase (JAK) is a family of cytoplasmic non-receptor tyrosine kinases that includes four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling through the JAK-STAT pathway, which regulates the transcription of several genes involved in inflammatory, immune, and cancer conditions. Targeting the JAK family kinases with small-molecule inhibitors has proved to be effective in the treatment of different types of diseases.

Structure-based design, synthesis, and biological evaluation of novel piperine-resveratrol hybrids as antiproliferative agents targeting SIRT-2.

A series of novel piperine-resveratrol hybrids 5a-h was designed, synthesized, and structurally elucidated by IR, and H, C, and F NMR. Antiproliferative activities of 5a-h were evaluated by NCI against sixty cancer cell lines. Compound 5b, possessing resveratrol pharmacophoric phenolic moieties, showed a complete cell death against leukemia HL-60 (TB) and Breast cancer MDA-MB-468 with growth inhibition percentage of -0.

New 1,2,4-oxadiazole/pyrrolidine hybrids as topoisomerase IV and DNA gyrase inhibitors with promising antibacterial activity.

A series of hybridized pyrrolidine compounds with a 1,2,4-oxadiazole moiety were synthesized to develop effective molecules against the enzymes DNA gyrase and topoisomerase IV (Topo IV). Compounds 8-20 were developed based on a previously disclosed series of compounds from our lab, but with small structural modifications in the hopes of increasing the compounds' biological activity. In comparison to novobiocin, with IC  = 170 nM, the findings of the DNA gyrase inhibitory assay revealed that compounds 16 and 17 were the most potent of all synthesized derivatives, with IC values of 180 and 210 nM, respectively.

Discovery of novel oxazole-based macrocycles as anti-coronaviral agents targeting SARS-CoV-2 main protease.

We have discovered a family of synthetic oxazole-based macrocycles to be active against SARS-CoV-2. The synthesis, pharmacological properties, and docking studies of the compounds are reported in this study. The structure of the new macrocycles was confirmed by NMR spectroscopy and mass spectrometry.

Novel 1,5-diaryl pyrazole-3-carboxamides as selective COX-2/sEH inhibitors with analgesic, anti-inflammatory, and lower cardiotoxicity effects.

COX-2 selective drugs have been withdrawn from the market due to cardiovascular side effects, just a few years after their discovery. As a result, a new series of 1,5-diaryl pyrazole carboxamides 19-31 was synthesized as selective COX-2/sEH inhibitors with analgesic, anti-inflammatory, and lower cardiotoxic properties. The target compounds were synthesized and tested in vitro against COX-1, COX-2, and sEH enzymes.

Design, Synthesis, Biological Evaluation, and Computational Studies of Novel Tri-Aryl Imidazole-Benzene Sulfonamide Hybrids as Promising Selective Carbonic Anhydrase IX and XII Inhibitors.

A novel series of tri-aryl imidazole derivatives - carrying benzene sulfonamide moiety has been designed for their selective inhibitory against hCA and activity. Six compounds were found to be potent and selective CA IX inhibitors with the order of > > > > > (Ki = 0.3-1.

Design, synthesis, and biological evaluation of novel EGFR inhibitors containing 5-chloro-3-hydroxymethyl-indole-2-carboxamide scaffold with apoptotic antiproliferative activity.

New EGFR inhibitor series of fifteen 5-chloro-3-hydroxymethyl-indole-2-carboxamide derivatives has been designed, synthesized, and tested for antiproliferative activity against a panel of cancer cell lines. The results showed that p-substituted phenethyl derivatives 10, 11, 13, 15 and 17-19 showed superior antiproliferative activity compared to their m-substituted counterparts 12, 14, 16 and 20. Compounds 15, 16, 19 and 20 displayed promising EGFR inhibitory activity as well as an increase in caspase 3 levels.

Wasp Venom Biochemical Components and Their Potential in Biological Applications and Nanotechnological Interventions.

Wasps, members of the order Hymenoptera, are distributed in different parts of the world, including Brazil, Thailand, Japan, Korea, and Argentina. The lifestyles of the wasps are solitary and social. Social wasps use venom as a defensive measure to protect their colonies, whereas solitary wasps use their venom to capture prey.

The use of Verbrugge forceps for reduction of the posterior column element in displaced acetabular fractures: clinical and radiological evaluation.

Purpose: Different reduction techniques and tools are described to facilitate anatomical reduction of acetabular fractures. However, maintenance of reduction, plate placement, and fracture fixation remain a challenge owing to the large surface area occupied by the available reduction tools. This study aims at radiological and functional assessment of the effectiveness of a novel reduction technique for the posterior column element in displaced acetabular fractures.

Symphyseal plate with trans-symphyseal cross-screws for fixation of tile-type B1 pelvic ring injuries: radiological and functional evaluation.

Introduction: Failure to neutralize the different physiological forces acting on the inferior as well as the superior regions of the pubic symphysis, the long healing time, is blamed for the repeated failures of conventional superior symphyseal plating.

Material And Methods: A three years prospective case series study between January 2017 and December 2019 was done, to evaluate the radiological and the functional outcomes, using Matta/Tornetta and Majeed criteria respectively, of the combination of trans-symphyseal cross-screws configuration and superior symphyseal plate in Tile-type B1 pelvic injuries.

Results: Thirty patients, 18 with anteroposterior compression type II and 12 with type III, with a mean follow-up of 20 months ±5 were included.

Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.

Herein we describe our efforts to develop novel anti-inflammatory/analgesic agents devoid of known cardiovascular drawbacks. In doing so, two 1,5-diarylpyrazole series of urea linked (9a-f) and amide linked (11a-f) compounds were synthesized and evaluated in vitro as dual COX-2/sEH inhibitors using recombinant enzyme assays. The in vivo anti-inflammatory and analgesic activities were then examined using reported animal models.

Treatment of non-united femoral neck fracture by a novel subtrochanteric angulation lateral translation valgus osteotomy (SALVA osteotomy).

Purpose: The ideal treatment of non-united and neglected fracture neck femur in the young adult still remains unclear and is characterized by many biological and biomechanical challenges.

Methods: Twenty-one patients with non-united or neglected fracture neck femur aged between 19 and 50 years were treated by a novel subtrochanteric valgus osteotomy and were followed up for a mean of 26.7 months.

Role of arthroscopy for the diagnosis and management of post-traumatic hip pain: a prospective study.

The current published literature regarding the role of hip arthroscopy in the diagnosis and management of post-traumatic hip pain is still limited. Therefore, we conducted the present prospective study to determine the value of hip arthroscopy in the diagnosis and management of various causes of hip pain after traumatic conditions. The present study included a prospective cohort of 17 patients with symptomatic post-traumatic hip pain.

Pyrrolizine-5-carboxamides: Exploring the impact of various substituents on anti-inflammatory and anticancer activities.

Towards optimization of the pyrrolizine-5-carboxamide scaffold, a novel series of six derivatives (4a-c and 5a-c) was prepared and evaluated for their anti-inflammatory, analgesic and anticancer activities. The (EZ)-7-cyano-6-((4-hydroxybenzylidene)amino)-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine-5-carboxamide (4b) and (EZ)-6-((4-chlorobenzylidene)-amino)-7-cyano-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine-5-carboxamide (5b) bearing the electron donating methyl group showed the highest anti-inflammatory activity while (EZ)-6-((4-chlorobenzylidene)amino)-7-cyano-N-phenyl-2,3-dihydro-1H-pyrrolizine-5-carboxamide (5a) was the most active analgesic agent. Cytotoxicity of the new compounds was evaluated against the MCF-7, A2780 and HT29 cancer cell lines using the MTT assay.

Design, Synthesis and Antiproliferative Evaluation of Novel 1,2,4-Triazole/Schiff Base Hybrids with EGFR and B-RAF Inhibitory Activities.

Background: 1,2,4-triazoles possess a broad spectrum of biological activities such as analgesic, antimicrobial, antitubercular, anti-inflammatory and antineoplastic activities. This heterocycle and their derivatives were included into a wide variety of therapeutically interesting drugs. Hence, it is of great interest to explore new 1,2,4-triazoles as cytotoxic agents targeting EGFR, B-Raf kinases.

Anti-inflammatory indomethacin analogs endowed with preferential COX-2 inhibitory activity.

The undeniable indomethacin potency has always suffered serious obstacles such as gastric damage. Continuous attempts to develop potent yet safe indomethacin analogs have never ceased. Herein are new indole derivatives and , which were synthesized via Fisher indole reaction, evaluated for both their anti-inflammatory activities using rat paw edema method and their cyclooxygenase inhibitory activities.

Synthesis, anticancer activity and molecular modeling studies of 1,2,4-triazole derivatives as EGFR inhibitors.

A series of novel compounds carrying 1,2,4-triazole scaffold were prepared and evaluated for their antiproliferative activities against NCI 60 cell line. Compounds 10 (a, c), 11 (a-d), and 14 (a-e) were selected for evaluation at single concentration of 10 μM towards panel of sixty cancer cell lines. Some of nitric oxide (NO) donating triazole/oxime hybrids 11a-d showed antiproliferative activity better than their corresponding ketones.