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Fulltext Psychometric properties of the environmental factors' questionnaire for undergraduate medical students taking online learning during COVID-19 pandemic: a cross-sectional study

Taleb OK, Siti-Azrin AH, Sarimah A, Abusafia AH, Baharuddin KA, Wan-Nor-Asyikeen WA

BMC Med Educ, 2023 May 22;23(1):356.
PMID: 37217957 DOI: 10.1186/s12909-023-04314-0

BACKGROUND: Environmental factors are important for students' learning during online classes, especially during a pandemic, such as COVID-19. This study aimed to validate the environmental factors' questionnaire during online learning.
METHODS: A total of 218 undergraduate medical students at the Health Campus, Universiti Sains Malaysia, participated in a cross-sectional study that involved an online survey. Environmental factor scales were assessed with the nine-item lighting, noise, and temperature (LNT) scale and the six-item technology scale. Analysis was performed using confirmatory factor analysis (CFA).
RESULTS: The English version of the LNT scale with nine items and three factors showed a good fit to the data, with no item deleted. For LNT, the composite reliability (CR) was 0.81, 0.81, and 0.84, respectively, while the average variance extracted (AVE) was 0.61, 0.59, and 0.6, respectively. The English version of the technology scale, with six items and one factor, also showed a good fit to the data, with no item deleted. The CR was 0.84, and the AVE was 0.51.
CONCLUSIONS: The results provide psychometric evidence for environmental questionnaire scales in evaluating the factors associated with online learning among Malaysian university medical students. All items were retained and confirmed to fit the sample data.
Fulltext Single-fed broadband CPW-fed circularly polarized implantable antenna for sensing medical applications

Butt AD, Khan J, Ahmad S, Ghaffar A, Abdullah Al-Gburi AJ, Hussein M

PLoS One, 2023;18(4):e0280042.
PMID: 37053176 DOI: 10.1371/journal.pone.0280042

Biomedical telemetry relies heavily on implantable antennas. Due to this, we have designed and tested a compact, a circularly polarized, a low-profile biomedical implantable antenna that operate in the 2.45 GHz ISM band. In order to keep the antenna compact, modified co-planar waveguide (CPW) technology is used. Slotted rectangular patch with one 45-degree angle slot and truncated little patch on the left end of the ground plane generate a frequency-range antenna with circular polarization. Using a 0.25-millimeter-thick Roger Duroid-RT5880 substrate with a thickness of εr = 2.2, tanδ = 0.0009 provides flexibility. The volume of the antenna is 21 mm x 13.5 mm x 0.254 mm (0.25λg × 0.16λg × 0.003λg). The antenna covers 2.35-2.55 GHz (200 MHz) in free space and 1.63-1.17 GHz (1.17 GHz) in epidermal tissue. With skin tissue that has more bandwidth, the (x and y)-axis bends of the antenna are also simulated via the simulation. Bended antenna simulations and measurements show excellent agreement. At 2.45 GHz, the skin-like gel had -10dB impedance and 3dB axial ratio (AR) bandwidths of 47.7 and 53.8%, respectively. The ultimate result is that the SAR values are 0.78 W/kg in skin over 1 g of bulk tissue, as determined by simulations. The suggested SAR values are lower than the FCC's maximum allowable limit (FCC). This antenna is small enough to be implanted in the body, making it perfect for biomedical applications.
Correction: ChatGPT in pharmacy practice: a cross-sectional exploration of Jordanian pharmacists' perception, practice, and concerns

Abu Hammour K, Alhamad H, Al-Ashwal FY, Halboup A, Abu Farha R, Abu Hammour A

J Pharm Policy Pract, 2023 Oct 30;16(1):129.
PMID: 37904185 DOI: 10.1186/s40545-023-00640-2
Synthesis, molecular docking and biological potentials of new 2-(4-(2-chloroacetyl) piperazin-1-yl)-N-(2-(4-chlorophenyl)-4-oxoquinazolin-3(4H)-yl)acetamide derivatives

Mehta S, Kumar S, Marwaha RK, Narasimhan B, Ramasamy K, Lim SM, et al.

BMC Chem, 2019 Dec;13(1):113.
PMID: 31517312 DOI: 10.1186/s13065-019-0629-0

In the present study, a series of 2-(4-(2-chloroacetyl)piperazin-1-yl)-N-(2-(4-chlorophenyl)-4-oxoquinazolin-3(4H)-yl)acetamide derivatives was synthesized and its chemical structures were confirmed by physicochemical and spectral characteristics. The synthesized compounds were evaluated for their in vitro antimicrobial (tube dilution technique) and anticancer (MTT assay) activities along with molecular docking study by Schrodinger 2018-1, maestro v11.5. The antimicrobial results indicated that compounds 3, 8, 11 and 12 displayed the significant antimicrobial activity and comparable to the standards drugs (ciprofloxacin and fluconazole). The anticancer activity results indicated that compound 5 have good anticancer activity among the synthesized compounds but lower active than the standard drugs (5-fluorouracil and tomudex). Molecular docking study demonstrated that compounds 5 and 7 displayed the good docking score with better anticancer potency within the binding pocket and these compounds may be used as a lead for rational drug designing for the anticancer molecules.
Preliminary assessment of the NACA0021 trailing edge wedge for wind turbine application

Abdalkarem AAM, Ansaf R, Muzammil WK, Ibrahim A, Harun Z, Fazlizan A

Heliyon, 2023 Nov;9(11):e21193.
PMID: 37942161 DOI: 10.1016/j.heliyon.2023.e21193

The airfoil blade is the primary component of a wind turbine, and its aerodynamic properties play a crucial role in determining the energy conversion efficiency of these blades. Many researchers have proposed different airfoil modifications intending to enhance the aerodynamic characteristics and limit the unsteady interaction with the atmospheric boundary layer. This study evaluates the benefits of mounting wedge tails (WTs) on the trailing edge of an airfoil. The aerodynamic characteristics of a 2-D, steady-state NACA 0021 airfoil featuring the wedge tails (WT) and fish wedge tails (FWT) were studied computationally by employing the shear stress transport (SST) k-ω turbulence model. Different WT and FWT configurations were studied at various wedge length (L) to wedge height (H) ratios, L/H, at the airfoil's trailing edge. The effects of different L/H ratios, including L/H > 1, L/H = 1, and L/H
ChatGPT in pharmacy practice: a cross-sectional exploration of Jordanian pharmacists' perception, practice, and concerns

Abu Hammour K, Alhamad H, Al-Ashwal FY, Halboup A, Abu Farha R, Abu Hammour A

J Pharm Policy Pract, 2023 Oct 03;16(1):115.
PMID: 37789443 DOI: 10.1186/s40545-023-00624-2

OBJECTIVES: The purpose of this study is to find out how much pharmacists know and have used ChatGPT in their practice. We investigated the advantages and disadvantages of utilizing ChatGPT in a pharmacy context, the amount of training necessary to use it proficiently, and the influence on patient care using a survey.
METHODS: This cross-sectional study was carried out between May and June 2023 to assess the potential and problems that pharmacists observed while integrating chatbots powered by AI (ChatGPT) in pharmacy practice. The correlation between perceived benefits and concerns was evaluated using Spearman's rho correlation due to the data's non-normal distribution.Any pharmacists licensed by the Jordanian Pharmacists Association were included in the study. A convenient sampling technique was used to choose the participants, and the study questionnaire was distributed utilizing an online medium (Facebook and WhatsApp). Anyone who expressed interest in taking part was given a link to the study's instructions so they may read them before giving their electronic consent and accessing the survey.
RESULTS: The potential advantages of ChatGPT in the pharmacy practice were widely acknowledged by the participants. The majority of participants (69.9%) concurred that educational material about pharmacy items or therapeutic areas can be provided using ChatGPT, with 66.9% of respondents believing that ChatGPT is a machine learning algorithm. Concerns about the accuracy of AI-generated responses were also prevalent. More than half of the participants (55.7%) raised the possibility that AI systems such as ChatGPT could pick up on and replicate prejudices and discriminatory patterns from the data they were trained on. Analysis shows a statistically significant positive link, albeit a minor one, between the perceived advantages of ChatGPT and its drawbacks (r = 0.255, p
Fulltext Solar irradiation prediction using empirical and artificial intelligence methods: A comparative review

Nawab F, Abd Hamid AS, Ibrahim A, Sopian K, Fazlizan A, Fauzan MF

Heliyon, 2023 Jun;9(6):e17038.
PMID: 37484325 DOI: 10.1016/j.heliyon.2023.e17038

Solar irradiation data is essential for the feasibility of solar energy projects. Notably, the intermittent nature of solar irradiation influences solar energy use in all forms, whether energy or agriculture. Accurate solar irradiation prediction is the only solution to effectively use solar energy in different forms. The estimation of solar irradiation is the most critical factor for site selection and sizing of solar energy projects and for selecting a suitable crop selection for the area. But the physical measurement of solar irradiation, due to the cost and technology involved, is not possible for all locations across the globe. Numerous techniques have been implemented to predict solar irradiation for this purpose. The two types of approaches that are most frequently employed are empirical techniques and artificial intelligence (AI). Both approaches have demonstrated good accuracy in various places of the world. To find out the best method, a thorough review of research articles discussing solar irradiation prediction has been done to compare different methods for solar irradiation prediction. In this paper, articles predicting solar irradiation using AI and empirical published from 2017 to 2022 have been reviewed, and both methods have been compared. The review showed that AI methods are more accurate than empirical methods. In empirical models, modified sunshine-based models (MSSM) have the highest accuracy, followed by sunshine-based (SSM) and non-sunshine-based models (NSM). The NSM has a little lower accuracy than MSSM and SSM, but the NSM can give good results in sunshine data unavailability. Also, the literature review confirmed that simple empirical models could predict accurately, and increasing the empirical model's polynomial order cannot improve results. Artificial neural networks (ANN) and Hybrid models have the highest accuracy among AI methods, followed by support vector machine (SVM) and adaptive neuro-fuzzy inference system (ANFIS). The increase in efficiency by hybrid models is minimal, but the complexity of models requires very sophisticated programming knowledge. ANN's most important input factors are maximum and minimum temperatures, temperature differential, relative humidity, clearness index and precipitation.
Fulltext A comprehensive review of security threats and solutions for the online social networks industry

Nawaz NA, Ishaq K, Farooq U, Khalil A, Rasheed S, Abid A, et al.

PeerJ Comput Sci, 2023;9:e1143.
PMID: 37346522 DOI: 10.7717/peerj-cs.1143

The term "cyber threats" refers to the new category of hazards that have emerged with the rapid development and widespread use of computing technologies, as well as our growing reliance on them. This article presents an in-depth study of a variety of security and privacy threats directed at different types of users of social media sites. Furthermore, it focuses on different risks while sharing multimedia content across social networking platforms, and discusses relevant prevention measures and techniques. It also shares methods, tools, and mechanisms for safer usage of online social media platforms, which have been categorized based on their providers including commercial, open source, and academic solutions.
Fulltext Distinct Optical and Structural (Nanoyarn and Nanomat-like Structure) Characteristics of Zinc Oxide Nanofilm Derived by Using Salvia officinalis Leaves Extract Made without and with PEO Polymer

Alrajhi AH, Ahmed NM, Halim MM, Altowyan AS, Azmi MN, Almessiere MA

Materials (Basel), 2023 Jun 21;16(13).
PMID: 37444824 DOI: 10.3390/ma16134510

This paper reports the optical properties of zinc oxide nanofilm fabricated by using organic natural products from Salvia officinalis leaves (SOL) extract and discusses the effect of the nanocrystal (NC) structure (nanoyarn and nanomat-like structure) on nanofilm optical properties. The surface-active layer of the nanofilm of ZnO nanoparticles (ZnO NPs) was passivated with natural organic SOL leaves hydrothermally, then accumulated on zinc oxide nanorods (ZnO NRs). The nanofilms were fabricated (with and without PEO) on glass substrate (at 85 °C for 16 h) via chemical solution deposition (CSD). The samples were characterized by UV-vis, PL, FESEM, XRD, and TEM measurements. TEM micrographs confirmed the nucleation of ZnO NPs around 4 nm and the size distribution at 1.2 nm of ZnO QDs as an influence of the quantum confinement effect (QCE). The nanofilms fabricated with SOL surfactant (which works as a capping agent for ZnO NPs) represent distinct optoelectronic properties when compared to bulk ZnO. FESEM images of the nanofilms revealed nanoyarn and nanomat-like structures resembling morphologies. The XRD patterns of the samples exhibited the existence of ZnO nanocrystallites (ZnO NCs) with (100), (002), and (101) growth planes. The nanofilms fabricated represented a distinct optical property through absorption and broad emission, as the optical energy band gap reduced as the nanofilms annealed (at 120 ℃). Based on the obtained results, it was established that phytochemicals extracted from organic natural SOL leaves have a distinct influence on zoic oxide nanofilm fabrication, which may be useful for visible light spectrum trapping. The nanofilms can be used in photovoltaic solar cell applications.
Do natural resources affect environmental quality in MINT Economies? The role of tourism and financial development

Faisal F, Rahman SU, Ali A, Sulimany HGH, Bazhair AH, Pervaiz R

Environ Sci Pollut Res Int, 2023 Oct;30(47):103958-103971.
PMID: 37691062 DOI: 10.1007/s11356-023-29520-7

With the growing nature of the ecological footprint, research studies focus on exploring new determinants of environmental degradation. Moreover, the role of natural resources and energy consumption in environmental quality has gained much attention in the literature. However, tourism raises the demand for energy consumption and extraction of natural resources. This research study investigates the influence of natural resources, tourism, and renewable energy in MINT countries, using novel Cross-Sectional Auto Regressive Distributive Lag (CS-ARDL) methodological techniques and employing yearly data from 1995 to 2018. The study also applied recently developed Kónya (Econ Model 23:978-992, 2006) causality to identify the causal relationship between the variables of the heterogenous panel. The result shows that tourism, natural resources, and economic growth are positively associated with the ecological footprint in the long-run. However, renewable energy consumption negatively impacts ecological footprint in both in short-run and the long-run. Further, the study explored a bidirectional causality between economic growth and ecological footprint in MINT countries. Finally, based on the empirical results, the study recommends that the authorities in MINT countries revisit their tourism, natural resources, and economic activities policies to enhance the environmental quality and reduce the ecological footprint.
Fulltext A Fusion-Based Machine Learning Approach for the Prediction of the Onset of Diabetes

Nadeem MW, Goh HG, Ponnusamy V, Andonovic I, Khan MA, Hussain M

Healthcare (Basel), 2021 Oct 18;9(10).
PMID: 34683073 DOI: 10.3390/healthcare9101393

A growing portfolio of research has been reported on the use of machine learning-based architectures and models in the domain of healthcare. The development of data-driven applications and services for the diagnosis and classification of key illness conditions is challenging owing to issues of low volume, low-quality contextual data for the training, and validation of algorithms, which, in turn, compromises the accuracy of the resultant models. Here, a fusion machine learning approach is presented reporting an improvement in the accuracy of the identification of diabetes and the prediction of the onset of critical events for patients with diabetes (PwD). Globally, the cost of treating diabetes, a prevalent chronic illness condition characterized by high levels of sugar in the bloodstream over long periods, is placing severe demands on health providers and the proposed solution has the potential to support an increase in the rates of survival of PwD through informing on the optimum treatment on an individual patient basis. At the core of the proposed architecture is a fusion of machine learning classifiers (Support Vector Machine and Artificial Neural Network). Results indicate a classification accuracy of 94.67%, exceeding the performance of reported machine learning models for diabetes by ~1.8% over the best reported to date.
Fabrication of amine-functionalized and multi-layered PAN-(TiO2)-gelatin nanofibrous wound dressing: In-vitro evaluation

Khan R, Haider S, Khan MUA, Haider A, Razak SIA, Hasan A, et al.

Int J Biol Macromol, 2023 Dec 31;253(Pt 5):127169.
PMID: 37783243 DOI: 10.1016/j.ijbiomac.2023.127169

The development of advanced multifunctional wound dressings remains a major challenge. Herein, a novel multilayer (ML) electrospun nanofibers (NFs) wound dressing based on diethylenetriamine (DETA) functionalized polyacrylonitrile (PAN), TiO2 nanoparticles (NPs) coating (Ct), and bioderived gelatin (Gel) was developed for potential applications in wound healing. The ML PAN-DETA-Ct-Gel membrane was developed by combining electrospinning, chemical functionalization, synthesis, and electrospray techniques, using a layer-by-layer method. The ML PAN-DETA-Ct-Gel membrane is comprised of an outer layer of PAN-DETA as a barrier to external microorganisms and structural support, an interlayer TiO2 NPs (Ct) as antibacterial function, and a contact layer (Gel) to improve biocompatibility and cell viability. The NFs membranes were characterized by scanning electron microscopy (SEM), surface profilometry, BET analysis, and water contact angle techniques to investigate their morphology, surface roughness, porosity, and wettability. The ML PAN-DETA-Ct-Gel wound dressing exhibited good surface roughness, porosity, and better wettability. Cell morphology, proliferation, and viability were determined using fibroblasts (3T3), and antibacterial assays were performed against six pathogens. The ML PAN-DETA-Ct-Gel NFs membrane showed good cell morphology, proliferation, viability, and antibacterial activity compared with other membranes. This new class of ML NFs membranes offers a multifunctional architecture with adequate biocompatibility, cell viability, and antibacterial activity.
Histological Characteristics on the Testes of Mud Spiny Lobster, Panulirus polyphagus (Herbst, 1793)

Nor Fatihah S, Muhd-Farouk H, Amin-Safwan A, Hafiz Mahsol H, Ikhwanuddin M

Pak J Biol Sci, 2017;20(7):365-371.
PMID: 29023069 DOI: 10.3923/pjbs.2017.365.371

BACKGROUND AND OBJECTIVE: Mud spiny lobsters, Panulirus polyphagus (P. polyphagus) are one of the most important fisheries resources now-a-days due to quality that it's possessed. However, there is still lack of in-depth study about this species mainly on males testicular characteristics and sexual maturity size. Therefore, the present study was carried out to investigate the histological characteristics on the testes and sexual maturity sizes of mud spiny lobster, Panulirus polyphagus.
MATERIALS AND METHODS: The testes were dissected out and fixed in 10% buffered formalin solution for 11 h, dehydrated in 70% alcohol and lastly placed in tissue processor for 18±1 h at 60°C. The tissues blocks were cut at the thickness of 4 μm on a rotary microtome. Stained tissues were taken under Advance Microscope (Nikon Eclipse 80i Nomarski DIC). Collected data were analyzed using Microsoft Excel 2013. Data were presented as mean±standard deviation. Statistical analyses were done using one-way ANOVA using SPSS (Version 22).
RESULTS: These lobules of mature P. polyphagus were formed via different germinative lineage cells such as spermatogonia, spermatocytes, spermatids and spermatozoa. The histological characteristics of testes showed that the process of spermatogenesis went through the stages of four testes maturation which were spermatogonia I and II, spermatocytes I and II, spermatids and spermatozoa stages within different body weight of P. polyphagus. It was found that there were significant difference between body weight and carapace length to the testicular maturation stages (one-way ANOVA and p = 0.000).
CONCLUSION: The results of this experiment indicated that males P. polyphagus have four stages of testes maturation and can be considered to have fully mature testes that ready for fertilization at 452 g body weight (BW) and 107 mm carapace length (CL) or more.
Fulltext A lightweight and robust authentication scheme for the healthcare system using public cloud server

Abbasi IA, Jan SU, Alqahtani AS, Khan AS, Algarni F

PLoS One, 2024;19(1):e0294429.
PMID: 38289970 DOI: 10.1371/journal.pone.0294429

Cloud computing is vital in various applications, such as healthcare, transportation, governance, and mobile computing. When using a public cloud server, it is mandatory to be secured from all known threats because a minor attacker's disturbance severely threatens the whole system. A public cloud server is posed with numerous threats; an adversary can easily enter the server to access sensitive information, especially for the healthcare industry, which offers services to patients, researchers, labs, and hospitals in a flexible way with minimal operational costs. It is challenging to make it a reliable system and ensure the privacy and security of a cloud-enabled healthcare system. In this regard, numerous security mechanisms have been proposed in past decades. These protocols either suffer from replay attacks, are completed in three to four round trips or have maximum computation, which means the security doesn't balance with performance. Thus, this work uses a fuzzy extractor method to propose a robust security method for a cloud-enabled healthcare system based on Elliptic Curve Cryptography (ECC). The proposed scheme's security analysis has been examined formally with BAN logic, ROM and ProVerif and informally using pragmatic illustration and different attacks' discussions. The proposed security mechanism is analyzed in terms of communication and computation costs. Upon comparing the proposed protocol with prior work, it has been demonstrated that our scheme is 33.91% better in communication costs and 35.39% superior to its competitors in computation costs.
Fulltext MESMERIC: Machine Learning-Based Trust Management Mechanism for the Internet of Vehicles

Wang Y, Mahmood A, Sabri MFM, Zen H, Kho LC

Sensors (Basel), 2024 Jan 29;24(3).
PMID: 38339580 DOI: 10.3390/s24030863

The emerging yet promising paradigm of the Internet of Vehicles (IoV) has recently gained considerable attention from researchers from academia and industry. As an indispensable constituent of the futuristic smart cities, the underlying essence of the IoV is to facilitate vehicles to exchange safety-critical information with the other vehicles in their neighborhood, vulnerable pedestrians, supporting infrastructure, and the backbone network via vehicle-to-everything communication in a bid to enhance the road safety by mitigating the unwarranted road accidents via ensuring safer navigation together with guaranteeing the intelligent traffic flows. This requires that the safety-critical messages exchanged within an IoV network and the vehicles that disseminate the same are highly reliable (i.e., trustworthy); otherwise, the entire IoV network could be jeopardized. A state-of-the-art trust-based mechanism is, therefore, highly imperative for identifying and removing malicious vehicles from an IoV network. Accordingly, in this paper, a machine learning-based trust management mechanism, MESMERIC, has been proposed that takes into account the notions of direct trust (encompassing the trust attributes of interaction success rate, similarity, familiarity, and reward and punishment), indirect trust (involving confidence of a particular trustor on the neighboring nodes of a trustee, and the direct trust between the said neighboring nodes and the trustee), and context (comprising vehicle types and operating scenarios) in order to not only ascertain the trust of vehicles in an IoV network but to segregate the trustworthy vehicles from the untrustworthy ones by means of an optimal decision boundary. A comprehensive evaluation of the envisaged trust management mechanism has been carried out which demonstrates that it outperforms other state-of-the-art trust management mechanisms.
Fulltext HLD-DDoSDN: High and low-rates dataset-based DDoS attacks against SDN

Bahashwan AA, Anbar M, Manickam S, Issa G, Aladaileh MA, Alabsi BA, et al.

PLoS One, 2024;19(2):e0297548.
PMID: 38330004 DOI: 10.1371/journal.pone.0297548

Software Defined Network (SDN) has alleviated traditional network limitations but faces a significant challenge due to the risk of Distributed Denial of Service (DDoS) attacks against an SDN controller, with current detection methods lacking evaluation on unrealistic SDN datasets and standard DDoS attacks (i.e., high-rate DDoS attack). Therefore, a realistic dataset called HLD-DDoSDN is introduced, encompassing prevalent DDoS attacks specifically aimed at an SDN controller, such as User Internet Control Message Protocol (ICMP), Transmission Control Protocol (TCP), and User Datagram Protocol (UDP). This SDN dataset also incorporates diverse levels of traffic fluctuations, representing different traffic variation rates (i.e., high and low rates) in DDoS attacks. It is qualitatively compared to existing SDN datasets and quantitatively evaluated across all eight scenarios to ensure its superiority. Furthermore, it fulfils the requirements of a benchmark dataset in terms of size, variety of attacks and scenarios, with significant features that highly contribute to detecting realistic SDN attacks. The features of HLD-DDoSDN are evaluated using a Deep Multilayer Perception (D-MLP) based detection approach. Experimental findings indicate that the employed features exhibit high performance in the detection accuracy, recall, and precision of detecting high and low-rate DDoS flooding attacks.
Fulltext Synthesis, molecular docking and biological evaluation of bis-pyrimidine Schiff base derivatives

Kumar S, Lim SM, Ramasamy K, Vasudevan M, Shah SAA, Selvaraj M, et al.

Chem Cent J, 2017 Sep 18;11(1):89.
PMID: 29086867 DOI: 10.1186/s13065-017-0322-0

BACKGROUND: Heterocyclic pyrimidine nucleus, which is an essential base component of the genetic material of deoxyribonucleic acid, demonstrated various biological activities. A series of bis-pyrimidine Schiff bases were synthesized and screened for its antimicrobial and anticancer potentials. The molecular docking study was carried to find the interaction between active molecules with receptor.
RESULTS: The structures of synthesized bis-pyrimidine Schiff bases were confirmed by spectral studies. The synthesized bis-pyrimidine derivatives were evaluated for their antimicrobial activity (MIC = µmol/mL) against selected Gram positive; Gram negative bacterial and fungal strains by tube dilution method. The anticancer activity (IC50 = µmol/mL) of the synthesized compounds was determined against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B (SRB) assay. Molecular docking studies provided information regarding the binding mode of active bis-pyrimidine Schiff bases with the cyclin-dependent kinase 8 (CDK8) receptor.
CONCLUSIONS: The antimicrobial screening results indicated that compounds, q1 (MICbs = 0.83 µmol/mL), q16 (MICan = 1.54 µmol/mL and MICec = 0.77 µmol/mL), q1 and q19 (MICca = 0.41 µmol/mL) and q20 (MIC = 0.36 µmol/mL) are the most active ones. Compounds q1 (IC50 = 0.18 µmol/mL) have emerged as potent anticancer molecule against human colorectal carcinoma cancer cell line than the reference drug, 5-fluorouracil. Molecular docking studies indicated that compound q1 (the most active molecule) has the maximum hydrogen bond interaction (four) and π-π stacking (three) network among the bis-pyrimidine Schiff bases. Graphical abstract Graphical illustration of predicted binding mode of bis-pyrimidine Schiff bases in the active site of CDK8. a. Compound 1 (magenta color), b. Compound 5 (green color), c. Compound 8 (red color), d. Compound 13 (split pea color).
Fulltext Synthesis, in vitro urease inhibitory potential and molecular docking study of benzofuran-based-thiazoldinone analogues

Taha M, Rahim F, Ullah H, Wadood A, Farooq RK, Shah SAA, et al.

Sci Rep, 2020 06 30;10(1):10673.
PMID: 32606439 DOI: 10.1038/s41598-020-67414-7

In continuation of our work on enzyme inhibition, the benzofuran-based-thiazoldinone analogues (1-14) were synthesized, characterized by HREI-MS, 1H and 13CNMR and evaluated for urease inhibition. Compounds 1-14 exhibited a varying degree of urease inhibitory activity with IC50 values between 1.2 ± 0.01 to 23.50 ± 0.70 µM when compared with standard drug thiourea having IC50 value 21.40 ± 0.21 µM. Compound 1, 3, 5 and 8 showed significant inhibitory effects with IC50 values 1.2 ± 0.01, 2.20 ± 0.01, 1.40 ± 0.01 and 2.90 ± 0.01 µM respectively, better than the rest of the series. A structure activity relationship (SAR) of this series has been established based on electronic effects and position of different substituents present on phenyl ring. Molecular docking studies were performed to understand the binding interaction of the compounds.
Fulltext Bis-pyrimidine acetamides: design, synthesis and biological evaluation

Kumar S, Lim SM, Ramasamy K, Vasudevan M, Shah SAA, Narasimhan B

Chem Cent J, 2017 Aug 08;11(1):80.
PMID: 29086907 DOI: 10.1186/s13065-017-0312-2

BACKGROUND: In the past few years, increased resistance of microorganisms towards antimicrobial agents become a serious health problem, so there is a need for the discovery of new antimicrobial agents. On the other hand, bis-pyrimidines possess various types of biological activity. In view of this, in the present study we have designed and synthesized a new series of bis-pyrimidine acetamides by Claisen-Schmidt condensation and screened for its in vitro antimicrobial and anticancer activities.
RESULTS: The synthesized bis-pyrimidine acetamide derivatives were confirmed by IR, (1)H/(13)C-NMR, Mass spectral studies as well C, H, N analyses. The synthesized compounds were evaluated for their in vitro antimicrobial potential against Gram positive (Staphylococcus aureus and Bacillus subtilis); Gram negative (Escherichia coli, Pseudomonas aeruginosa and Salmonella enterica) bacterial and fungal (Candida albicans and Aspergillus niger) strains by tube dilution technique and the minimum inhibitory concentration (MIC) recorded in µmol/mL was comparable to reference drugs, cefadroxil (antibacterial) and fluconazole (antifungal). The in vitro anticancer activity (IC50 value) determined against human colorectal carcinoma (HCT116) cancer cell line by Sulforhodamine B (SRB) technique and 5-fluorouracil used as reference drug.
CONCLUSIONS: The biological study demonstrated that compounds 3, 13, 16, 17 and 18 were found to be most active antimicrobial agents with best MIC values than the cefadroxil (antibacterial) and fluconazole (antifungal) and compounds 12, 16 and 18 found to have better anticancer activity against human colorectal carcinoma (HCT116) cancer cell line with best IC50 value than the 5-fluorouracil (anticancer). Graphical abstract SAR of bis-pyrimidine acetamides.
Fulltext Urinary Tract Infection among Renal Transplant Recipients in Yemen

Gondos AS, Al-Moyed KA, Al-Robasi AB, Al-Shamahy HA, Alyousefi NA

PLoS One, 2015;10(12):e0144266.
PMID: 26657128 DOI: 10.1371/journal.pone.0144266

Urinary tract infection (UTI) is the most common complication following kidney transplantation (KT), which could result in losing the graft. This study aims to identify the prevalence of bacterial UTI among KT recipients in Yemen and to determine the predisposing factors associated with post renal transplantation UTI. A cross sectional study included of 150 patients, who underwent KT was conducted between June 2010 and January 2011. A Morning mid-stream urine specimen was collected for culture and antibiotic susceptibility test from each recipient. Bacterial UTI was found in 50 patients (33.3%). The prevalence among females 40.3% was higher than males 29%. The UTI was higher in the age group between 41-50 years with a percentage of 28% and this result was statistically significant. Predisposing factors as diabetes mellitus, vesicoureteral reflux, neurogenic bladder and polycystic kidney showed significant association. High relative risks were found for polycystic kidney = 13.5 and neurogenic bladder = 13.5. The most prevalent bacteria to cause UTI was Escherichia coli represent 44%, followed by Staphylococcus saprophyticus 34%. Amikacin was the most effective antibiotic against gram-negative isolates while Ciprofloxacin was the most effective antibiotic against Staphylococcus saprophyticus. In conclusion, there is high prevalence of bacterial UTI among KT recipients in Yemen. Diabetes mellitus, vesicoureteral reflux, neurogenic bladder, polycystic kidney and calculi were the main predisposing factors.

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