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  1. A sustainable method for oxidizing phenanthrene in tropical soil using natural iron as a catalyst in a slurry phase reactor with persulfate assistance
    Qutob M, Rafatullah M, Muhammad SA, Siddiqui MR, Alam M
    Environ Sci Process Impacts, 2024 Jul 08.
    PMID: 38973648 DOI: 10.1039/d4em00328d
    The presence of impurities is a significant restriction to the use of natural iron minerals as catalysts in the advanced oxidation process (AOP), especially if applied for soil remediation. This study evaluated the catalytic activity of tropical soil, which has relatively low impurities and naturally contains iron, for the remediation of phenanthrene (PHE) contamination. The system showed good performance, and the best result was 81% PHE removal after 24 h under experimental conditions of pH 7, [PHE]0 = 300 mg/50 g soil, temperature 55 °C, air flow = 260 mL min-1, and [persulfate]0 = 20 mg kg-1, while the mineralization was 61%. Nevertheless, certain limitations were noted in the soil matrix following the remediation procedure, including the appearance of cracks in the soil aggregate, reduction in the crystal size of the soil particles, and decline in the iron and aluminium contents. The results confirmed that the radicals play a major role in the remediation process. SO4˙- was more dominant than O2˙-, while HO˙ played a minor role. Additionally, the by-products were detected by gas chromatography-mass spectroscopy (GC-MS), and the degradation pathway of PHE is proposed. Toxicity assessment tests were performed by using a computational method. In spite of the challenges, this research achieved notable progress in soil remediation, taking a significant step forward in implementing the AOP without catalysts to activate oxidants and remove PHE within the soil. Also, this approach supports sustainability by reducing the need for extra materials and providing an environmentally friendly way of soil remediation.
  2. Measuring spatial inequalities in maternal and child mortalities in Pakistan: evidence from geographically weighted regression
    Muhammad FS, Shahabudin SM, Talib MBA
    BMC Public Health, 2024 Aug 16;24(1):2229.
    PMID: 39152373 DOI: 10.1186/s12889-024-19682-5
    BACKGROUND: In developing countries, the death probability of a child and mother is more significant than in developed countries; these inequalities in health outcomes are unfair. The present study encompasses a spatial analysis of maternal and child mortalities in Pakistan. The study aims to estimate the District Mortality Index (DMI), measure the inequality ratio and slope, and ascertain the spatial impact of numerous factors on DMI scores across Pakistani districts.

    METHOD: This study used micro-level household datasets from multiple indicator cluster surveys (MICS) to estimate the DMI. To find out how different the DMI scores were, the inequality ratio and slope were used. This study further utilized spatial autocorrelation tests to determine the magnitude and location of the spatial dependence of the clusters with high and low mortality rates. The Geographically Weighted Regression (GWR) model was also applied to examine the spatial impact of socioeconomic, environmental, health, and housing attributes on DMI.

    RESULTS: The inequality ratio for DMI showed that the upper decile districts are 16 times more prone to mortalities than districts in the lower decile, and the districts of Baluchistan depicted extreme spatial heterogeneity in terms of DMI. The findings of the Local Indicator of Spatial Association (LISA) and Moran's test confirmed spatial homogeneity in all mortalities among the districts in Pakistan. The H-H clusters of maternal mortality and DMI were in Baluchistan, and the H-H clusters of child mortality were seen in Punjab. The results of GWR showed that the wealth index quintile has a significant spatial impact on DMI; however, improved sanitation, handwashing practices, and antenatal care adversely influenced DMI scores.

    CONCLUSION: The findings reveal a significant disparity in DMI and spatial relationships among all mortalities in Pakistan's districts. Additionally, socioeconomic, environmental, health, and housing variables have an impact on DMI. Notably, spatial proximity among individuals who are at risk of death occurs in areas with elevated mortality rates. Policymakers may mitigate these mortalities by focusing on vulnerable zones and implementing measures such as raising public awareness, enhancing healthcare services, and improving access to clean drinking water and sanitation facilities.

  3. A Psychometric Properties of the Malay-version Police Stress Questionnaire
    Irniza R, Emilia ZA, Muhammad Saliluddin S, Nizam Isha AS
    Malays J Med Sci, 2014 Jul;21(4):42-50.
    PMID: 25977621 MyJurnal
    BACKGROUND: Police Stress Questionnaire (PSQ) was developed to measure police-specific stressors. The present study was the first to have translated the PSQ to Malay. This study aims to test the reliability, construct validity, and component structure of the Malay-version PSQ.

    METHODS: A set of survey consisted of the Malay-version PSQ, General Health Questionnaire (GHQ-12), Job Content Questionnaire (JCQ), Global Stress Questionnaire (GSQ) and General Self-rated Health (GSRH) were distributed to 300 traffic police officers in Kuala Lumpur and all traffic police officers in a few districts of Pahang and Negeri Sembilan.

    RESULTS: The response rate was 65.5% (N = 262). The reported Cronbach's alpha coefficient was 0.93 for Operational PSQ (PSQ-Op) and 0.94 for Organisational PSQ (PSQ-Org). Findings indicated that the PSQ had positive construct validity with the GSRH, GSQ, and GHQ. After excluding four factors related to lifestyles, all police-specific stressors were highly loaded (0.50) in one component.

    CONCLUSION: It is confirmed that the Malay-version PSQ, excluding the four factors related to lifestyle, was uni-dimensional, reliable, and a valid questionnaire. This study proffers a potentially better instrument for assessing the stressors among Malaysian police.

  4. Impact of Article Page Count and Number of Authors on Citations in Disability Related Fields: A Systematic Review Article
    Ahmed A, Adam M, Ghafar NA, Muhammad M, Ebrahim NA
    Iran J Public Health, 2016 Sep;45(9):1118-1125.
    PMID: 27957456
    BACKGROUND: Citation metrics and total publications in a field has become the gold standard for rating researchers and viability of a field. Hence, stimulating demand for citation has led to a search for useful strategies to improve performance metric index. Meanwhile, title, abstract and morphologic qualities of the articles attract researchers to scientific publications. Yet, there is relatively little understanding of the citation trend in disability related fields. We aimed to provide an insight into the factors associated with citation increase in this field. Additionally, we tried to know at what page number an article might appear attractive to disability researchers needs. Thus, our focus is placed on the article page count and the number of authors contributing to the fields per article.

    METHODS: To this end, we evaluated the quantitative characteristics of top cited articles in the fields with a total citation (≥50) in the Web of Science (WoS) database. Using one-way independent ANOVA, data extracted spanning a period of 1980-2015 were analyzed, while the non-parametric data analysis uses Kruskal-Walis test.

    RESULTS: Articles with 11 to 20 pages attract more citations followed by those within the range of zero to 10. Articles with upward 21 pages are the least cited. Surprisingly, articles with more than two authors are significantly (P<0.05) less cited and the citation decreases as the number of authors increased.

    CONCLUSION: Collaborative studies enjoy wider utilization and more citation, yet discounted merit of additional pages and limited collaborative research in disability field is revealed in this study.

  5. Assessing and anticipating environmental challenges in Lahore, Pakistan: future implications of air pollution on sustainable development and environmental governance
    Nasar-U-Minallah M, Jabbar M, Zia S, Perveen N
    Environ Monit Assess, 2024 Aug 30;196(9):865.
    PMID: 39212804 DOI: 10.1007/s10661-024-12925-3
    Urban environment and air quality are changing primarily due to land use land cover (LULC) changes, economic activity, and urbanization. Air pollution has been increasingly acknowledged as a major issue for cities due to its extensive effects on health and well-being. As the second most populous city in the country, Lahore faces alarming levels of air pollutants, which induced this study to focus on the pervasive issue of air pollution in Lahore. For this, the study collected air pollutants data from the Environmental Protection Department of Punjab and analyzed them using the ARIMA model. In the research results, both the observed data and predictive models uncovered concerning trends in pollutant concentrations, ultimately portraying a concerning picture for air quality management. Carbon monoxide (CO) levels show a consistent rise, surpassing Pakistan's environmental standards by 2025. Similarly, nitrogen dioxide (NO2) concentrations escalate, exceeding prescribed standards. Ground-level ozone (O3) also demonstrates a substantial increase, surpassing standards by 2025. Both PM2.5 and PM10 exhibit marked upward trends, projected to exceed recommended limits, particularly PM10 throughout the study year. The Air Quality Index exhibits an observable upward trend, fluctuating between 70 and 442 from 2015 to 2020. Similarly, a positive correlation was found between population growth and land use conversion into residential areas. Projections suggest a continuous increase, potentially hitting a severe level of 500 during winter by 2025. These findings point to an impending air pollution crisis, demanding urgent action to address the hazardous situation in the city. The study recommends that urban air pollution should be reduced, and the negative health effects of air pollution should be minimized using vegetation barriers, screens, and greening initiatives. Strict regulations and monitoring initiatives need to be put in place in big cities to monitor pollution and vegetation.
  6. Eight-and-a-Half Syndrome Secondary to Acute Brainstem Infarction
    Muhammad H, Chan WS, Jaafar J, Wan Hitam WH
    Cureus, 2024 Jul;16(7):e65138.
    PMID: 39171063 DOI: 10.7759/cureus.65138
    Eight-and-a-half syndrome is a rare neuro-ophthalmologic condition, which is characterized by ipsilateral horizontal gaze palsy, internuclear ophthalmoplegia (INO), and ipsilateral lower motor neuron facial palsy. We report a case of eight-and-a-half syndrome secondary to acute brainstem infarction. A 55-year-old gentleman with underlying diabetes mellitus and hypertension presented with a sudden onset of double vision in the right lateral gaze for one day. On examination, there was a limitation in the left eye horizontal eye movement with limited right eye adduction. Further neurological examination revealed left lower motor neuron facial nerve palsy. Magnetic resonance imaging (MRI) of the brain showed an acute infarct involving the left side of the thalamus extending to the left side of the midbrain, pons, and medulla. He was diagnosed with eight-and-a-half syndrome secondary to acute brainstem infarction. The patient was referred to the neuromedical team, where he was treated with anti-platelet medications. He showed gradual improvement on follow-up and had complete resolution of ophthalmoplegia after three months. There was only minimal residual facial nerve weakness. Eight-and-a-half syndrome has a localizing value to the dorsal tegmentum of the pons. It requires thorough neurological examination and imaging studies for accurate diagnosis and management. This case highlights the potential for a significant recovery in patients with eight-and-a-half syndrome when timely and appropriate treatment is administered.
  7. Fulltext Quality of Life and Illness Acceptance among End-Stage Renal Disease (ESRD) Patients on Hemodialysis: The Moderating Effect of Death Anxiety during COVID-19 pandemic
    Mushtaque I, Awais-E-Yazdan M, Zahra R, Anas M
    Omega (Westport), 2024 Jun;89(2):567-586.
    PMID: 35254867 DOI: 10.1177/00302228221075202
    The purpose of the study was to examine the quality of life and illness acceptance among ESRD patients with the moderating effects of death anxiety. The cross-sectional design was incorporated. The sample was comprised of 240 participants. Individuals with ESRD on hemodialysis were approached above 20 years of age. A self-administered questionnaire was used for data collection. The results revealed that COVID-19 has a significant impact on the quality of life of patients and their illness acceptance. Covid-19 affected the general health of patients, their psychological health, as well as their social relationships. The results also confirmed that death anxiety negatively moderates the relationship between quality of life and illness acceptance among ESRD patients. This study will shed light on the need to provide appropriate psychosocial care as well as supportive therapies to people with end-stage renal disease who are experiencing mental distress during and after the COVID-19 outbreak.
  8. Fulltext Levosulpiride for Premature Ejaculation: A Systematic Review and Meta-Analysis
    Arshad A, Irfan M, Inam M, Hussain NHN, Ismail SB
    Am J Mens Health, 2022;16(5):15579883221124832.
    PMID: 36154321 DOI: 10.1177/15579883221124832
    Premature ejaculation (PE) is one of the major causes of sexual dysfunction. Levosulpiride is an off-label medicine used to treat PE, but no review on its efficacy exists. A systematic review and meta-analysis was performed to determine the efficacy of levosulpiride in treating PE. Databases PubMed, Science Direct, and Google Scholar were searched. Randomized control trials (RCTs) comparing levosulpiride with placebo or other medicine were selected. Odds ratio (OR) of improved intravaginal ejaculation latency time (IELT) was calculated. A total of 97 articles were retrieved from database search, of which only four RCTs containing 203 men met the selection criteria. All four RCTs were included in systematic review while only two were included in meta-analysis. A high selection and detection bias was found in both of these studies. Meta-analysis also showed the odds of improving IELT in PE patients using levosulpiride to be significantly higher (p < .05) compared with those who used placebo, OR: 100.81, 95% confidence interval (CI) [13.12-774.90], I2 = 0%. Odds of improving IELT for > 5 min (500% improvement) were also significantly higher (p < .05) compared with the placebo groups (OR: 38.88, 95% CI [5.12-295.29], I2 = 0%). The odds of improving IELT for > 1 min, but < 5 min were also significantly higher (p < .05) than placebo groups (OR: 32.84, 95% CI [4.15-259.75], I2 = 0%). Levosulpiride improved IELT, but even so, limited studies are available on this topic. Additional research is thus required to support the present review's findings.
  9. Remediation of benzo[α]pyrene contaminated soil using iron naturally bearing in tropical soil: A new frontier in catalyst-free in soil remediation
    Qutob M, Rafatullah M, Muhammad SA, Siddiqui MR, Alam M
    Chemosphere, 2024 Sep 06;364:143291.
    PMID: 39243904 DOI: 10.1016/j.chemosphere.2024.143291
    Nature iron is considered one of the promising catalysts in advanced oxidation processes (AOPs) that are utilized for soil remediation from polycyclic aromatic hydrocarbons (PAHs). However, the existence of anions, cations, and organic matter in soils considered impurities that restricted the utilization of iron that was harnessed naturally in the soil matrix and reduced the catalytic performance. In this regard, tropical soil naturally containing iron and relatively poor with impurities was artificially contaminated with 100 mg/50 g benzo[α]pyrene (B[α]P) and remediated using a slurry phase reactor supported with persulfate (PS). The results indicated that tropical soil containing iron and relatively poor with impurities capable of activating the oxidants and formation of radicals which successfully degraded B[α]P. The optimum removal result was 86% and obtained under the following conditions airflow = 260 mL/min, temperature 55 °C, pH 7, and [PS]0 = 1.0 g/L, at the same experimental conditions soil organic matter (SOM) mineralization was 48%. After the remediation process, there was a significant reduction in iron and aluminum contents, which considered the drawbacks of this system. Experiments to scavenge reactive species highlighted O2•- and SO4•- as the main radicals that oxidized B[α]P. Additionally, monitoring of by-products post-remediation aimed to assess toxicity and elucidate degradation pathways. Mutagenicity tests yielded positive results for two B[α]P by-products. The toxicity tests considered were the lethal concentration of 50% (LC50 96 h) for fat-head minnows revealed that all B[α]P by-products were less toxic than the parent pollutant itself. This research marks a significant advancement in soil remediation by advancing the use of the AOP method, removing the requirement for additional catalysts in the AOP system for the removal of B[α]P from soil.
  10. Fulltext Clinical and Sociodemographic Predictors of the Quality of Life among Patients with Type 2 Diabetes Mellitus on the East Coast of Peninsular Malaysia
    Jusoh Z, Tohid H, Omar K, Muhammad NA, Ahmad S
    Malays J Med Sci, 2018 Feb;25(1):84-95.
    PMID: 29599638 MyJurnal DOI: 10.21315/mjms2018.25.1.10
    Background: The quality of life (QoL) describes the multidimensional self-perceived well-being of a person, which is an important diabetes outcome. This study aimed to measure the QoL scores among patients with type 2 diabetes mellitus (T2DM), as well as their clinical and sociodemographic predictors.

    Methods: This cross-sectional study involved 180 randomly sampled patients at a primary care clinic on the East Coast of Peninsular Malaysia. A self-administered questionnaire containing the Audit of Diabetes Dependent Quality of Life-18 (ADDQoL-18) was used.

    Results: Most of the respondents (96.7%) were Malay, with a median (interquartile range, IQR) age of 54.0 (14.0) years old. The majority of them were females (60.0%), married (81.1%) and from low-income families (63.3%), who attained a secondary education or lower (75.6%). Only 49.4% of them were employed. The mean (standard deviation, SD) ADDQoL-18 average weighted impact score was -4.58 (2.21) and all 18 domains were negatively affected, particularly the living condition, family life and working life. The multiple linear regression analysis showed that the age (adjusted B = 0.05,P= 0.004) and insulin use (adjusted B = -0.84,P= 0.011) were QoL predictors.

    Conclusion: T2DM negatively impacts the patient's QoL in all aspects of their life. The QoL improvement with age suggests that the older patients had accepted and adapted to their illness. The need to improve the QoL among insulin users was also highlighted.
    Study site: Klinik Kesihatan, Malaysia
  11. Synthesis of novel inhibitors of α-glucosidase based on the benzothiazole skeleton containing benzohydrazide moiety and their molecular docking studies
    Taha M, Ismail NH, Lalani S, Fatmi MQ, Atia-Tul-Wahab, Siddiqui S, et al.
    Eur J Med Chem, 2015 Mar 6;92:387-400.
    PMID: 25585009 DOI: 10.1016/j.ejmech.2015.01.009
    In an effort to design and synthesize a new class of α-glucosidase inhibitor, we synthesized benzothiazole hybrid having benzohydrazide moiety (5). Compound 5 was reacted with various substituted aryl aldehyde to generate a small library of compounds 6-35. Synthesis of compounds was confirmed by the spectral information. These compounds were screened for their α-glucosidase activity. They showed a varying degree of α-glucosidase inhibition with IC50 values ranging between 5.31 and 53.34 μM. Compounds 6, 7, 9-16, 19, 21-30, 32-35 showed superior activity as compared to standard acarbose (IC50 = 906 ± 6.3 μM). This has identified a new class of α-glucosidase inhibitors. The predicted physico-chemical properties indicated the drug appropriateness for most of these compounds, as they obey Lipinski's rule of five (RO5). A hybrid B3LYP density functional theory (DFT) was employed for energy, minimization of 3D structures for all synthetic compounds using 6-311 + G(d,p) basis sets followed by molecular docking to explore their interactions with human intestinal C- and N-terminal domains of α-glucosidase. All compounds bind to the prospective allosteric site of the C- terminal domain, and consequently, may be considered as mixed inhibitors. It was hypothesized that both the dipole moment and H-bond interactions govern the biological activation of these compounds.
  12. Semiconducting composite oxide Y2CuO4-5CuO thin films for investigation of photoelectrochemical properties
    Ahmed S, Mansoor MA, Mazhar M, Söhnel T, Khaledi H, Basirun WJ, et al.
    Dalton Trans, 2014 Jun 14;43(22):8523-9.
    PMID: 24756425 DOI: 10.1039/c4dt00719k
    An octa-nuclear heterobimetallic complex [Y2Cu6Cl0.7(dmae)6(OAc)7.3(OH)4(H2O)2]·3H2O·0.3CH3C6H5 (dmae = dimethylaminoethanoate; OAc = acetato) was synthesized, characterized by melting point analysis, elemental analysis, FT-IR, and single crystal X-ray diffraction analysis and implemented at 600 °C under an oxygen atmosphere for the deposition of Y2CuO4-5CuO composite thin films by aerosol assisted chemical vapor deposition (AACVD). The chemical composition and surface morphology of the deposited thin film have been determined by X-ray diffraction, scanning electron microscopy and energy dispersive X-ray analysis that suggest the formation of impurity-free crystallite mixtures of the Y2CuO4-5CuO composite, with well-defined evenly distributed particles in the size range of 19-24 nm. An optical band gap energy of 1.82 eV was estimated by UV-visible spectrophotometry. PEC studies show that under illumination with a 150 W halogen lamp and at a potential of 0.8 V, a photocurrent density of 9.85 μA cm(-2) was obtained.
  13. Fulltext Evaluation of Potential Drug-Drug Interactions with Antidepressants in Two Tertiary Care Hospitals
    Rafi MS, Naqvi SB, Khan MU, Fayyaz M, Ashraf N, Khan MA, et al.
    J Clin Diagn Res, 2015 Jul;9(7):FC05-8.
    PMID: 26393139 DOI: 10.7860/JCDR/2015/13437.6207
    Limited resources of healthcare system and high use of antidepressants have raised some serious concerns regarding proper surveillance system of prescribed medicines. Not much literature is available from Pakistan regarding the potential drug-drug interactions (pDDIs) associated with antidepressants.
  14. Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation
    Zha GF, Zhang CP, Qin HL, Jantan I, Sher M, Amjad MW, et al.
    Bioorg Med Chem, 2016 05 15;24(10):2352-9.
    PMID: 27083471 DOI: 10.1016/j.bmc.2016.04.015
    A series of new α,β-unsaturated carbonyl-based cyclohexanone derivatives was synthesized by simple condensation method and all compounds were characterized by using various spectroscopic techniques. New compounds were evaluated for their effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These compounds were also screened for in vitro cytotoxicity and for inhibitory activity for self-induced Aβ1-42 aggregation. The effect of these compounds against amyloid β-induced cytotoxicity was also investigated. The findings of in vitro experiment revealed that most of these compounds exhibited potent inhibitory activity against AChE and self-induced Aβ1-42 aggregation. The compound 3o exhibited best AChE (IC50=0.037μM) inhibitory potential. Furthermore, compound 3o disassembled the Aβ fibrils produced by self-induced Aβ aggregation by 76.6%. Compounds containing N-methyl-4-piperidone linker, showed high acetylcholinesterase and self-induced Aβ aggregation inhibitory activities as compared to reference drug donepezil. The pre-treatment of cells with synthetic compounds protected them against Aβ-induced cell death by up to 92%. Collectively, these findings suggest that some compounds from this series have potential to be promising multifunctional agents for AD treatment and our study suggest the cyclohexanone derivatives as promising new inhibitors for AChE and BuChE, potentially useful to treat neurodegenerative diseases.
  15. Synthesis, α-glucosidase inhibitory, cytotoxicity and docking studies of 2-aryl-7-methylbenzimidazoles
    Taha M, Ismail NH, Imran S, Mohamad MH, Wadood A, Rahim F, et al.
    Bioorg Chem, 2016 Apr;65:100-9.
    PMID: 26894559 DOI: 10.1016/j.bioorg.2016.02.004
    Benzimidazole analogs 1-27 were synthesized, characterized by EI-MS and (1)HNMR and their α-glucosidase inhibitory activities were found out experimentally. Compound 25, 19, 10 and 20 have best inhibitory activities with IC50 values 5.30±0.10, 16.10±0.10, 25.36±0.14 and 29.75±0.19 respectively against α-glucosidase. Compound 6 and 12 has no inhibitory activity against α-glucosidase enzyme among the series. Further studies showed that the compounds are not showing any cytotoxicity effect. The docking studies of the compounds as well as the experimental activities of the compounds correlated well. From the molecular docking studies, it was observed that the top ranked conformation of all the compounds fit well in the active site of the homology model of α-glucosidase.
  16. Fulltext A System for True and False Memory Prediction Based on 2D and 3D Educational Contents and EEG Brain Signals
    Bamatraf S, Hussain M, Aboalsamh H, Qazi EU, Malik AS, Amin HU, et al.
    Comput Intell Neurosci, 2016;2016:8491046.
    PMID: 26819593 DOI: 10.1155/2016/8491046
    We studied the impact of 2D and 3D educational contents on learning and memory recall using electroencephalography (EEG) brain signals. For this purpose, we adopted a classification approach that predicts true and false memories in case of both short term memory (STM) and long term memory (LTM) and helps to decide whether there is a difference between the impact of 2D and 3D educational contents. In this approach, EEG brain signals are converted into topomaps and then discriminative features are extracted from them and finally support vector machine (SVM) which is employed to predict brain states. For data collection, half of sixty-eight healthy individuals watched the learning material in 2D format whereas the rest watched the same material in 3D format. After learning task, memory recall tasks were performed after 30 minutes (STM) and two months (LTM), and EEG signals were recorded. In case of STM, 97.5% prediction accuracy was achieved for 3D and 96.6% for 2D and, in case of LTM, it was 100% for both 2D and 3D. The statistical analysis of the results suggested that for learning and memory recall both 2D and 3D materials do not have much difference in case of STM and LTM.
  17. A novel five-step synthetic route to 1,3,4-oxadiazole derivatives with potent α-glucosidase inhibitory potential and their in silico studies
    Iftikhar M, Shahnawaz, Saleem M, Riaz N, Aziz-Ur-Rehman, Ahmed I, et al.
    Arch Pharm (Weinheim), 2019 Dec;352(12):e1900095.
    PMID: 31544284 DOI: 10.1002/ardp.201900095
    A series of new N-aryl/aralkyl derivatives of 2-methyl-2-{5-(4-chlorophenyl)-1,3,4-oxadiazole-2ylthiol}acetamide were synthesized by successive conversions of 4-chlorobenzoic acid (a) into ethyl 4-chlorobenzoate (1), 4-chlorobenzoylhydrazide (2) and 5-(4-chlorophenyl)-1,3,4-oxadiazole-2-thiol (3), respectively. The required array of compounds (6a-n) was obtained by the reaction of 1,3,4-oxadiazole (3) with various electrophiles (5a-n) in the presence of DMF (N,N-dimethylformamide) and sodium hydroxide at room temperature. The structural determination of these compounds was done by infrared, 1 H-NMR (nuclear magnetic resonance), 13 C-NMR, electron ionization mass spectrometry, and high-resolution electron ionization mass spectrometry analyses. All compounds were evaluated for their α-glucosidase inhibitory potential. Compounds 6a, 6c-e, 6g, and 6i were found to be promising inhibitors of α-glucosidase with IC50 values of 81.72 ± 1.18, 52.73 ± 1.16, 62.62 ± 1.15, 56.34 ± 1.17, 86.35 ± 1.17, 52.63 ± 1.16 µM, respectively. Molecular modeling and ADME (absorption, distribution, metabolism, excretion) predictions supported the findings. The current synthesized library of compounds was achieved by utilizing very common raw materials in such a way that the synthesized compounds may prove to be promising drug leads.
  18. Fulltext Exploring the linkage between PM2.5 levels and COVID-19 spread and its implications for socio-economic circles
    Ali SM, Malik F, Anjum MS, Siddiqui GF, Anwar MN, Lam SS, et al.
    Environ Res, 2021 02;193:110421.
    PMID: 33160973 DOI: 10.1016/j.envres.2020.110421
    A pneumonia-like disease of unknown origin caused a catastrophe in Wuhan city, China. This disease spread to 215 countries affecting a wide range of people. World health organization (WHO) called it a pandemic and it was officially named as Severe Acute Respiratory Syndrome Corona virus 2 (SARS CoV-2), also known as Corona virus disease (COVID-19). This pandemic compelled countries to enforce a socio-economic lockdown to prevent its widespread. This paper focuses on how the particulate matter pollution was reduced during the lockdown period (23 March to April 15, 2020) as compared to before lockdown. Both ground-based and satellite observations were used to identify the improvement in air quality of Pakistan with primary focus on four major cities of Lahore, Islamabad, Karachi and Peshawar. Both datasets have shown a substantial reduction in PM2.5 pollution levels (ranging from 13% to 33% in case of satellite observations, while 23%-58% in ground-based observations) across Pakistan. Result shows a higher rate of COVID-19 spread in major cities of Pakistan with poor air quality conditions. Yet more research is needed in order to establish linkage between COVID-19 spread and air pollution. However, it can be partially attributed to both higher rate of population density and frequent exposure of population to enhanced levels of PM2.5 concentrations before lockdown period.
  19. Fulltext Design, synthesis, and spasmolytic activity of thiophene-based derivatives via Suzuki cross-coupling reaction of 5-bromothiophene-2-carboxylic acid: their structural and computational studies
    Rasool N, Ikram HM, Rashid A, Afzal N, Hashmi MA, Khan MN, et al.
    Turk J Chem, 2020;44(5):1410-1422.
    PMID: 33488240 DOI: 10.3906/kim-1911-51
    In the current research work, a facile synthesis of a series of novel thiophene-based derivatives of 5-bromothiophene-2-carboxylic acid ( 1 ) have been synthesized. All analogs ( 5a - 5e , 10a - 10f ) were obtained from the coupling reaction of 5-bromothiophene-2-carboxylic acid ( 1 ) and different arylboronic acids with moderate-to-good yields under controlled and optimal conditions. The structures of the newly synthesized compounds were characterized through spectral analysis and their spasmolytic activity, and most of the compounds exhibited potentially good spasmolytic effect. Among the synthesized analogs, compound phenethyl 5-(3,4-dichlorophenyl)thiophene-2-carboxylate ( 10d ) particular showed an excellent spasmolytic effect with an EC 50 value of 1.26. All of the compounds were also studied for their structural and electronic properties by density functional theory (DFT) calculations. Through detailed insight into frontier molecular orbitals of the compounds and their different reactivity descriptors, it was found that the compounds 10c and 5c are the most reactive, while 10a is the most stable in the series. Furthermore, compounds 10c and 5c showed a very good NLO response with the highest β values.
  20. Formation of Antihyperlipidemic Nano-Ezetimibe from Volatile Microemulsion Template for Enhanced Dissolution Profile
    Saleem MA, Yasir Siddique M, Nazar MF, Khan SU, Ahmad A, Khan R, et al.
    Langmuir, 2020 07 14;36(27):7908-7915.
    PMID: 32551692 DOI: 10.1021/acs.langmuir.0c01016
    Nanostructures play an important role in targeting sparingly water-soluble drugs to specific sites. Because of the structural flexibility and stability, the use of template microemulsions (μEs) can produce functional nanopharmaceuticals of different sizes, shapes, and chemical properties. In this article, we report a new volatile oil-in-water (o/w) μE formulation comprising ethyl acetate/ethanol/brij-35/water to obtain the highly water-dispersible nanoparticles of an antihyperlipidemic agent, ezetimibe (EZM-NPs), to enhance its dissolution profile. A pseudoternary phase diagram was delineated in a specified brij-35/ethanol ratio (1:1) to describe the transparent, optically isotropic domain of the as-formulated μE. The water-dilutable μE formulation, comprising an optimum composition of ethyl acetate (18.0%), ethanol (25.0%), brij-35 (25.0%), and water (32.0%), showed a good dissolvability of EZM around 4.8 wt % at pH 5.2. Electron micrographs showed a fine monomodal collection of EZM-loaded μE droplets (∼45 nm) that did not coalesce even after lyophilization, forming small spherical EZM-NPs (∼60 nm). However, the maturity of nanodrug droplets observed through dynamic light scattering suggests the affinity of EZM to the nonpolar microenvironment, which was further supported through peak-to-peak correlation of infrared analysis and fluorescence measurements. Moreover, the release profile of the as-obtained EZM-nanopowder increased significantly >98% in 30 min, which indicates that a reduced drug concentration will be needed for capsules or tablets in the future and can be simply incorporated into the multidosage formulation of EZM.
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