16 research outputs found

    A one-pot Synthesis of Some New Heterocyclic Compounds Derived from Chalcones and Study of their Antitumor and Antimicrobial Activities

    Get PDF
    The aim of the present work is to efficiently synthesize promising novel antitumor and antimicrobial active heterocyclic compounds from chalcones 1a and 1b as a precursor which contain naphthalene moiety and indole or piperonal moiety, respectively, using conventional, ultrasonic and microwave irradiation techniques. The best yields and purity were afforded with the microwave irradiation technique. Reaction of 1a and 1b with the appropriate reagent gave the corresponding pyrazolines 2a, 2b, pyrimidine-2-thioneses 3a, 3b, oxazepines 4a, 4b, diazepines 5a, 5b, triazolo-pyrimidines 6a, 6b, and pyrimidine-2-thiols 7a, 7b derivatives. Compounds 7a, 7b were used to produce 8a, 8b. Moreover, pyrimidine-2-thione 3a was used to synthesize pyrimidin-2-ylthioacetic acid 9a, and 2-hydrazinylpyrido[2,3-d]pyrimidine derivative 10a which has been used as a functionalizing agent to produce compounds 11a-14a. The structural formulas of the synthesized compounds were confirmed by their spectral data; FT-IR, 1H NMR, 13C NMR and MS. Compounds 3a, 5a, 7a, 13a showed a very high activity as antitumor, whereas compounds 4a, 6a, and 13a showed high activity as antibacterial and antifungal agents

    Mechanical Thrombectomy for Acute Ischemic Stroke in Metastatic Cancer Patients: A Nationwide Cross-Sectional Analysis

    Get PDF
    BACKGROUND AND PURPOSE: Mechanical thrombectomy (MT) is the standard treatment for large vessel occlusion (LVO) acute ischemic stroke. Patients with active malignancy have an increased risk of stroke but were excluded from MT trials. METHODS: We searched the National Readmission Database for LVO patients treated with MT between 2016-2018 and compared the characteristics and outcomes of cancer-free patients to those with metastatic cancer (MC). Primary outcomes were all-cause in-hospital mortality and favorable outcome, defined as a routine discharge to home (regardless of whether home services were provided or not). Multivariate regression was used to adjust for confounders. RESULTS: Of 40,537 LVO patients treated with MT, 933 (2.3%) had MC diagnosis. Compared to cancer-free patients, MC patients were similar in age and stroke severity but had greater overall disease severity. Hospital complications that occurred more frequently in MC included pneumonia, sepsis, acute coronary syndrome, deep vein thrombosis, and pulmonary embolism (P\u3c0.001). Patients with MC had similar rates of intracerebral hemorrhage (20% vs. 21%) but were less likely to receive tissue plasminogen activator (13% vs. 23%, P\u3c0.001). In unadjusted analysis, MC patients as compared to cancer-free patients had a higher in-hospital mortality rate and were less likely to be discharged to home (36% vs. 42%, P=0.014). On multivariate regression adjusting for confounders, mortality was the only outcome that was significantly higher in the MC group than in the cancerfree group (P\u3c0.001). CONCLUSION: LVO patients with MC have higher mortality and more infectious and thrombotic complications than cancer-free patients. MT nonetheless can result in survival with good outcome in slightly over one-third of patients

    Impact of opioid-free analgesia on pain severity and patient satisfaction after discharge from surgery: multispecialty, prospective cohort study in 25 countries

    Get PDF
    Background: Balancing opioid stewardship and the need for adequate analgesia following discharge after surgery is challenging. This study aimed to compare the outcomes for patients discharged with opioid versus opioid-free analgesia after common surgical procedures.Methods: This international, multicentre, prospective cohort study collected data from patients undergoing common acute and elective general surgical, urological, gynaecological, and orthopaedic procedures. The primary outcomes were patient-reported time in severe pain measured on a numerical analogue scale from 0 to 100% and patient-reported satisfaction with pain relief during the first week following discharge. Data were collected by in-hospital chart review and patient telephone interview 1 week after discharge.Results: The study recruited 4273 patients from 144 centres in 25 countries; 1311 patients (30.7%) were prescribed opioid analgesia at discharge. Patients reported being in severe pain for 10 (i.q.r. 1-30)% of the first week after discharge and rated satisfaction with analgesia as 90 (i.q.r. 80-100) of 100. After adjustment for confounders, opioid analgesia on discharge was independently associated with increased pain severity (risk ratio 1.52, 95% c.i. 1.31 to 1.76; P < 0.001) and re-presentation to healthcare providers owing to side-effects of medication (OR 2.38, 95% c.i. 1.36 to 4.17; P = 0.004), but not with satisfaction with analgesia (beta coefficient 0.92, 95% c.i. -1.52 to 3.36; P = 0.468) compared with opioid-free analgesia. Although opioid prescribing varied greatly between high-income and low- and middle-income countries, patient-reported outcomes did not.Conclusion: Opioid analgesia prescription on surgical discharge is associated with a higher risk of re-presentation owing to side-effects of medication and increased patient-reported pain, but not with changes in patient-reported satisfaction. Opioid-free discharge analgesia should be adopted routinely

    Delayed versus early pushing during the second stage of labour in primigravidas under epidural anaesthesia with occipitoposterior malposition: a randomised controlled study

    No full text
    This randomised controlled trial aimed to compare the effect of early and delayed pushing during the second stage of labour in women with occipitoposterior (OP) malposition. It included 184 nulliparous women with OP position randomised to early pushing in which women were allowed to push within one hour after full cervical dilatation or delayed pushing in which women were asked not to push for maximum of three hours or start pushing when the vertex was visible. The primary outcome was successful vaginal delivery. The rate of spontaneous vaginal delivery was significantly higher in the early pushing group (80.4 vs. 60.9%, p=.004) while the rate of instrumental vaginal delivery (30.4 vs. 15.4%) and CS (8.7 vs. 4.3%) was significantly higher in the delayed pushing group. Women in the delayed pushing group showed a significantly longer duration of the second stage (129.4 ± 7.5 vs. 61.6 ± 15.3 minutes, p<.001) and shorter duration of pushing (219.8 ± 74.8 vs. 693.9 ± 145.2 seconds, p<.001) .The rate of 2nd and 3rd degree perineal lacerations (19.6 and 13% vs. 5.4 and 8.7% respectively, p=.013) and vaginal tears (41.3 vs. 8.7%, p<.001) was significantly higher in the early pushing group. We concluded that early pushing during the second stage of labour is associated with higher rates of spontaneous vaginal delivery and vaginal and perineal lacerations. Clinical trial registration NCT03121274.Impact Statement What is already known on this subject? Occipitoposterior malposition is common during delivery especially in primigravida and is associated with higher rates of instrumental delivery and caesarean section. It can be managed through early or delayed pushing. What the results of this study add? Early pushing is associated with higher rates of spontaneous vaginal delivery, perineal and vaginal tears, shorter duration of second stage of labour, shorter duration of pushing, lower rates of both instrumental vaginal delivery and caesarean section. What the implications are of these findings for clinical practice and/or further research? Early pushing during the second stage of labour is associated with higher rates of spontaneous vaginal delivery and vaginal and perineal lacerations in women with OP malposition and should be tried and not delaying the pushing

    An Intelligent Approach for Fair Assessment of Online Laboratory Examinations in Laboratory Learning Systems Based on Student’s Mouse Interaction Behavior

    No full text
    The COVID-19 pandemic has made the world focus on providing effective and fair online learning systems. As a consequence, this paper proposed a new intelligent, fair assessment of online examinations for virtual and remotely controlled laboratory experiments running through Laboratory Learning Systems. The main idea is to provide students with an environment similar to being physically present in a Laboratory while conducting practical experiments and exams and detecting cheating with high accuracy at a minimal cost. Therefore, an intelligent assessment module is designed to detect cheating students by analyzing their mouse dynamics using Artificial Intelligence. The mouse interaction behavior method was chosen because it does not require any additional resources, such as a camera and eye tribe tracker, to detect cheating. Various AI algorithms, such as KNN, SVC, Random Forest, Logistic Regression, XGBoost, and LightGBM have been used to classify student mouse behavior to detect cheating, and many metrics are used to evaluate their performance. Moreover, experiments have been conducted on students answering online laboratory experimentations while cheating and when answering the exams honestly. Experimental results indicate that the LightGBM AI algorithm achieves the best cheat detection results up to an accuracy of 90%, precision of 88%, and degree of separation of 95%

    A Generic AI-Based Technique for Assessing Student Performance in Conducting Online Virtual and Remote Controlled Laboratories

    No full text
    Due to the COVID-19 pandemic and the development of educational technology, e-learning has become essential in the educational process. However, the adoption of e-learning in sectors such as engineering, science, and technology faces a particular challenge as it needs a special Laboratory Learning Management System (LLMS) capable of supporting online lab activities through virtual and controlled remote labs. One of the most challenging tasks in designing such LLMS is how to assess a student&#x2019;s performance while an experiment is being conducted and how stuttering students can be automatically detected while experimenting and providing the appropriate assistance. For this, a generic technique based on Artificial Intelligence (AI) is proposed in this paper for assessing student performance while conducting online labs and implemented as a performance evaluation module in the LLMS. The performance evaluation module is designed to automatically detect the student performance during the experiment run time and triggers the LLMS virtual assistant service to provide struggling students with the appropriate help when they need it. Also, the proposed performance assessment technique is used during the lab exam sessions to support the automatic grading process conducted by the LLMS Auto-Grading Module. The proposed performance evaluation technique has been developed based on analyzing the student&#x2019;s mouse dynamics to work generally with any type of simulation or control software used by virtual or remote controlled laboratories; without the need for special interfacing. The study has been applied to a novel dataset built by the course instructors and students simulating a circuit on TinkerCad. Using mouse dynamics fetching, the system extracts features and evaluates them to determine if the student has built the experiment steps in the right way or not. A comparison study has been developed between different Machine Learning (ML) models and a number of performance metrics are calculated. The study confirmed that Artificial Neural Network (ANN) and Support Vector Machine (SVM) are the best models to be used for automatically evaluating student performance while conducting the online labs with a precision reaching up to 91&#x0025;

    Evaluation of clinical outcomes in children with intrahepatic cholestasis postpartial external biliary diversion: A single-center experience

    No full text
    Background: Severe pruritus caused by progressive familial intrahepatic cholestasis (PFIC) and Alagille syndrome (AGS) is refractory to medical treatment. Surgical interruption of the enterohepatic circulation is considered the mainstay of alleviating distressing symptoms and delaying cirrhosis. Aim and Objectives: This study aims to evaluate the short-term effect of partial external biliary diversion (PEBD) on pruritus, liver disease progression, patient's growth, and quality of life. Material and Methods: This prospective cohort study enrolled children with PFIC and AGS from July 2019 to July 2021, whose guardians consented to the PEBD procedure. A standard surgical approach was performed by a single surgeon. Outcomes were measured subjectively and objectively pre- and post-procedure using the pruritus 5-D itching score, Paediatric Quality of Life Inventory scale (PedsQL), growth parameters, bile acids level, and liver function tests. Patients' follow-up period ranged from 6 to 12 months. Results: Seven patients had PEBD procedure; five with PFIC and two with AGS. A significant improvement was detected in the 5-D itching score (p-value < 0.001), PedsQL (p-value < 0.001), and bile acids level (p-value 0.013). The preexisting growth failure was ameliorated. The downward trend in the bilirubin level was not significant. No influential difference in the other liver function tests occurred. No intra-operative complications encountered. Only one case had a post-operative stoma prolapse which was managed surgically. Conclusion: PEBD procedure could be considered as an effective and safe treatment options for intractable pruritus in patients with PFIC or AGS, providing preserved synthetic liver functions

    Evaluation of the Anti-Cancer Potential of Rosa damascena Mill. Callus Extracts against the Human Colorectal Adenocarcinoma Cell Line

    No full text
    Chemotherapy is an aggressive form of chemical drug therapy aiming to destroy cancer cells. Adjuvant therapy may reduce hazards of chemotherapy and help in destroying these cells when obtained from natural products, such as medical plants. In this study, the potential therapeutic effect of Rosa damascena callus crude extract produced in vitamin-enhanced media is investigated on colorectal cancer cell line Caco-2. Two elicitors, i.e., L-ascorbic acid and citric acid at a concentration of 0.5 g/L were added to the callus induction medium. Callus extraction and the GC&ndash;MS analysis of methanolic crude extracts were also determined. Cytotoxicity, clonogenicity, proliferation and migration of Caco-2 colorectal cancer cells were investigated using MTT cytotoxicity, colony-forming, Ki-67 flow cytometry proliferation and Migration Scratch assays, respectively. Our results indicated that L-ascorbic acid treatment enhanced callus growth parameters and improved secondary metabolite contents. It showed the least IC50 value of 137 ug/mL compared to 237 ug/mL and 180 ug/mL in the citric acid-treated and control group. We can conclude that R. damascena callus elicited by L-ascorbic acid improved growth and secondary metabolite contents as well as having an efficient antiproliferative, anti-clonogenic and anti-migratory effect on Caco-2 cancer cells, thus, can be used as an adjuvant anti-cancer therapy
    corecore