Synthesis of quinoline attached-furan-2(3H)-ones having anti-inflammatory and antibacterial properties with reduced gastro-intestinal toxicity and lipid peroxidation

A series of 3-[2-chloroquinolin-3-yl)methylene]-5-aryl-furan-2(3H)-ones {3(a-p)} were synthesized. The required 3-(substitutedbenzoyl) propionic acids {2(a-d)} were prepared under Friedal Craft acylation reaction conditions. The substituted 2-chloroquinoline-3-carbaldehydes {1(a-d)} were synthesized by reaction of substitutedphenylethanone-oxime with phosphorus oxychloride in presence of dimethyl formamide using the Vilsmeir Haack reaction method. These compounds were screened for their anti-inflammatory and antibacterial activities along with their ulcerogenic and lipid peroxidation potentials. The compounds that showed significant anti-inflammatory activity were further screened for their analgesic activity. The compounds were less toxic in terms of ulcerogenicity as compared to a standard, which was also supported by lipid peroxidation studies. The antibacterial activities were performed against Staphylococcus aureus and Escherichia coli. Compounds 3f, 3n and 3o showed significant activity against both S. aureus and E. coli having an MIC value of 6.25μg mL-1

An Overview on Execution of Green Chemistry as an Alternative Technique in Organic Synthesis

The implementation of green chemistry (GC) in various aspects of chemistry to overcome the problems of health, safety for workers, in addition to the environmental problems is associated with compounds from their manufacturing, use and disposition as waste. GC is a rapid promising branch of chemistry. GC is a manner that maximizes its benefits while removed its adverse impacts by the application of principles. The principles of GC focused on methods that deals with avoidance of waste, maximize atom economy, less harmful chemical formed, metathesis, synthesized safer chemicals, using safer solvents, auxiliaries, renewable Feedstocks, softer catalysts other than heavy metals, biocatalysts, avoid the formation of chemical derivatives, develop energy efficient synthesis, progress of safer chemistry methods for accident avoidance. GC is interested for research and alternative improvement on many practical phases of organic compounds synthesis. GC intended for less toxic solvents but in recent years new methods have been developed where organic synthesis can be performed without solvents, mild conditions and low energy consumption. New approaches have promoted the use of alternative methods or “green” solvents. The new field of “green” solvents in organic compounds synthesis has been extended and gives some idea about green solvent, green catalyst, and green techniques for green synthesis

Characterization of Thermal, Ionic Conductivity and Electrochemical Properties of Some p-Tosylate Anions-Based Protic Ionic Compounds

Kingdom of Saudi Arabia, Award Number (2-17-01-001-0042In the present work, six protic ionic liquid (PIL) compounds based on p-toluene sulfonic acid [PTSA] anion along with different cations viz. tetraethylenepentammonium [TEPA], triethy-lammonium [TEA], pyridinium [Py], N-methylpiperidinium [Pip], 1-methylimidazolium [Im], and N-methylpyrrolidinium [Pyrr] were synthesized using the standard neutralization reaction method. The structural characterization of these compounds was achieved using FTIR,1H and13C NMR spectroscopies. Thermal behavior was studied using differential scanning calorimetry to determine the melting point (Tm) and crystallization (Tc ) temperatures. Thermogravimetric analysis was carried out to determine the thermal stability and degradation temperatures (Tdec) and to ascertain the hygroscopic or hydrophobic nature of the synthesized compounds. Structural effects on the outcome of various properties were witnessed and discussed in detail. Electrochemical impedance spectroscopy was utilized to study the electrical transport properties of the PILs at different temperatures. Cyclic voltammetry was performed to analyze the electrochemical stability of these PILs. Low values of activation energy indicating easy proton transportation along with good electrochemical stability make the PILs a potential candidate for use in the preparation of polymer electrolytes membranes for fuel cell applications.publishersversionpublishe

Spectrum of neurological disorders in neurology outpatients clinics in urban and rural Sindh, Pakistan: a cross sectional study

Background: Neurological disorders are the most common cause of morbidity and mortality in developing countries. Available evidence on urban–rural differences on neurological diseases is scare in such countries. Our study objective was to determine the prevalence of neurological diseases in urban and rural tertiary care hospitals of Sindh, Pakistan. Methods: This was a cross sectional study conducted in selected urban and rural region of tertiary care hospitals of Sindh, Pakistan. The outpatients medical records of adults (18 years and above) was obtained from January 1st, 2014 to December 31st, 2014. Results: A total of 10,786 outpatients visit were recorded in this period. Mean age of the participants was 40.6 ± 15 years; majority was females 6104 (56.6%). About three-fourth of the patients were from rural hospital 7828 (72.6%). Common neurological diseases were headache disorders 3613 (33.4%), nerve and root lesion 2928 (27.1%), vascular diseases 1440 (13.3%), epilepsies 566 (5.2%), muscle disorders 424 (3.9%), psychiatric disorders 340 (3.1%) and CNS infection 303 (2.8%). Comparison between the urban and rural samples showed that ischaemic stroke (72.7% vs. 82%) and psychiatric disorders (2.1% vs. 3.5%) were more prevalent in rural area as compared to urban setting. Conclusion: Stroke, headache and nerve and root lesion are major causes of neurological disorders in urban and rural settings of Sindh, Pakistan. The policy and planning must be focus on primary care, preventive measures and the promotion of health

QT interval prolongation in people treated with bedaquiline for drug-resistant tuberculosis

Background: Bedaquiline (BDQ) is indeed recommended for treating multidrug-resistant tuberculosis (MDR-TB). However, it's essential to monitor patients receiving bedaquiline therapy closely because it has been associated with prolongation of the QTc interval. This study aimed to assess the association of bedaquiline to QT interval prolongation in DR-TB patients. Methods: This was an observational longitudinal study conducted in the Department of Respiratory Medicine in Chest Disease Hospital, Rajshahi, from August 2020 to February 2023.  A total of 44 MDR-TB patients were included in the study. Data analyses were done by using Statistical Package for Social Sciences (SPSS) version 25.0. Results: Out of 44 patients the majority 30(68.2%) patients belonged to age >40 years with a mean age of 49.3±15.6 years, and all patients were male. All MDR patients were detected by sputum Gene-Xpert, 44 (100%), and sputum for AFB culture was done in all patients, 44 (100%). QT level and QT changes were statistically significant for baseline and 24 weeks. Only one patient died in 2 weeks of follow-up (Table 3). Changes of QT >60 ms was found in 6 (13.6%) and ≤60 ms was 38 (86.4%). Age, sex, marital status, residence, educational status, occupational status, monthly income, chief complaints, co-morbidities, and using drug-causing QT prolongation were not statistically significant (p>0.05). Conclusions: Prolonged QT interval is in DR-TB patients who receive treatment using the bedaquiline regimen. We observed that with a moderate prolongation of QTc, there were no arrhythmias recorded and 1 death occurred due to acute MI

Potential of Scorpion (Scorpiops pseudomonatus) Venom in Diabetes Therapy: A Study on α-Amylase and α-Glucosidase Inhibition

Background: The increasing number of diabetes mellitus patients and the complications of its treatment using chemical medicine have made it necessary to look for new treatment options that can control blood glucose levels. Objective: To explore the possibility of using scorpion venom as an inhibitor of the essential enzymes that hydrolyze carbohydrates, glucosidase and amylase, which are important targets in diabetes treatment. Methodology: Scorpion (Scorpiops pseudomonatus) venom has been evaluated for α-amylase and α-glucosidase inhibitory activities using standardized assays. Venom from selected scorpion species has been assessed for inhibitory activity using in vitro biochemical assays. IC50 values have been determined to evaluate the inhibitory potency and specificity. Results: About 35 scorpion individual species were taken, and 0.3-0.5 milligrams of venom from every scorpion individual were collected. Significant inhibition of both α-amylase α-glucosidase and activities was shown in the results (Amylase: 9.230 ± 2.475 and Glucosidase: 2.753 ± 0.573 IC50 ± STD). Conclusion: According to the results, scorpion (Scorpiops pseudomonatus) venom has the potential to be a unique therapeutic method for controlling blood sugar levels, as it is a promising source of natural enzyme inhibitors

A Large Multi-Target Dataset of Common Bengali Handwritten Graphemes

Latin has historically led the state-of-the-art in handwritten optical character recognition (OCR) research. Adapting existing systems from Latin to alpha-syllabary languages is particularly challenging due to a sharp contrast between their orthographies. The segmentation of graphical constituents corresponding to characters becomes significantly hard due to a cursive writing system and frequent use of diacritics in the alpha-syllabary family of languages. We propose a labeling scheme based on graphemes (linguistic segments of word formation) that makes segmentation in-side alpha-syllabary words linear and present the first dataset of Bengali handwritten graphemes that are commonly used in an everyday context. The dataset contains 411k curated samples of 1295 unique commonly used Bengali graphemes. Additionally, the test set contains 900 uncommon Bengali graphemes for out of dictionary performance evaluation. The dataset is open-sourced as a part of a public Handwritten Grapheme Classification Challenge on Kaggle to benchmark vision algorithms for multi-target grapheme classification. The unique graphemes present in this dataset are selected based on commonality in the Google Bengali ASR corpus. From competition proceedings, we see that deep-learning methods can generalize to a large span of out of dictionary graphemes which are absent during training. Dataset and starter codes at www.kaggle.com/c/bengaliai-cv19.Comment: 15 pages, 12 figures, 6 Tables, Submitted to CVPR-2

Pain Perception and Rate of Canine Retraction Through Self- Ligating Brackets and Conventional Elastomeric Ligation System: A Split Mouth Study

Objective: To evaluate the rate of tooth movement and the pain perception via self-ligating (SL) and conventional elastomeric ligation brackets (CB) system. Material and Methods: This study has been conducted at the Orthodontic Department of Baqai Dental College, Baqai Medical University. The sample size of this study comprised 40 patients, falling between the age of 12-30 years without any sex discrimination. Shapiro-Wilk was used to check the distribution of data. Non-parametric Mann Whitney U test was applied to evaluate the pain associated with SL and CB brackets system. To analysis the canine retraction Wilcoxon test was applied for the comparison of CB and SL brackets system. For all statistical analyses, the p-value of <0.05 was considered significant. Results: Pain level associated with retraction via CB and SL shows significant differences. However, the rate of canine retraction via CB and SL shows no significant differences at stages T0-T1 and T1-T2. However, stage T2-T3 shows a significant difference. Conclusion: As pain during orthodontic treatment is mostly associated with the level of compression of the periodontal ligament, it may be hypothesized that lower frictional forces generate less compression of the periodontal ligament and blood vessels, and so alter the type of pain experienced