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3,5-Disubstituted Thiadiazine-2-thiones: New Cell-Cycle Inhibitors
Awwad A. Radwan,Tarek Aboul-Fadl,Abdullah Al-Dhfyan,Mohammed K. Abdel-Hamid,Abdullah A. Al-Badr 대한약학회 2012 Archives of Pharmacal Research Vol.35 No.1
Two series, a and b, of 3-cyclopentyl or (3-cyclohexyl)-5-substituted-3,4,5,6-tetrahydro-2H-1,3,5-thiadiazine-2-thiones (THTT) 2a-9a and 3b, 4b, 6b-9b, were synthesized to develop new cell cycle inhibitors. Variable and promising in vitro antiproliferative activities were shown with the synthesized THTT derivatives. Compound 5a with a 5-cyclopentyl group on position-3 and a glutamine residue on position-5 of the THTT moiety showed maximum activity (IC50 = 8.98 μM). Compound 5a possessed notable cell cycle disrupting and apoptotic activities with enhanced selectivity against cancer cells, suggesting the potential for the development of new selective cell cycle inhibitors. There is no evident relationship between the cytotoxic activity of the tested compounds and their lipophilicity. In addition, a pharmacophore based study was performed to explain the biological activity on structural bases. A successful model was generated with a good correlation with the observed activity.
Voluntary testing for COVID-19: perceptions and utilization among the inhabitants of Saudi Arabia
Ehab A. Abo-Ali,Ahmed Mousa,Rania Hussien,Shahad Mousa,Shayma Al-Rubaki,Mennatulla Omar,Badr Al-Haffashi,Abdullah Almilaibary 질병관리본부 2022 Osong Public Health and Research Persptectives Vol.13 No.3
Objectives: Voluntary testing (VT) plays a crucial role in the prevention and control of infectious diseases. The present study investigated the perceptions and utilization of VT services for coronavirus disease 2019 (COVID-19) among the inhabitants of Saudi Arabia.Methods: In total, 3,510 adult participants from all provinces of Saudi Arabia were recruited via a national online survey.Results: Of the 3,510 participants, 88.9% were aware of the testing services available to them and of those, more than half (59.5%) had used the VT services and 96.1% were satisfied with the services. Contact with a positive COVID-19 case was the top reason for accessing VT, while a lack of awareness about the availability of VT services was the top perceived limiting factor. A history of chronic health conditions, anxiety and/or depression, and previous symptoms suggestive of COVID-19 were found to be predictors of the utilization of VT services (odds ratio [OR] 1.55, 95% confidence interval [CI] 1.22−1.96; OR 1.48, 95% CI 1.16−1.88; and OR 3.31, 95% CI 2.77−3.95), respectively.Conclusion: The awareness of voluntary COVID-19 testing services was satisfactory among the Saudi Arabian population, but can be improved. Sociodemographic and health history predictors of the utilization of VT services were identified.
Single-nozzle Core-shell Electrospun Nanofibers of PVP/Dextran as Drug Delivery System
Meera Moydeen A.,Syed Ali Padusha M.,Badr M. Thamer,Anis Ahamed N.,Abdullah M. Al-Enizi,Hany El-Hamshary,Mohamed H. El-Newehy 한국섬유공학회 2019 Fibers and polymers Vol.20 No.10
Ciprofloxacin-loaded poly(vinylpyrrolidinone) (PVP) and dextran sulfate (Dex) (PVP/Dex) nanofibers wereprepared using the emulsion electrospinning method. The physical and morphological characteristics of the preparednanofibers were evaluated by conducting a Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy(SEM) and thermogravimetric analysis (TGA). The polymer-polymer and polymer-drug interactions were determined usingdifferential scanning calorimetry (DSC). Moreover, the formation of the core-shell structure was confirmed by transmissionelectron microscopy (TEM) and confocal laser microscopy. The sustained release behavior was evaluated using ultravioletvisible(UV-vis) spectroscopy, and its kinetic mechanism was investigated using Korsmeyer-Peppas, Peppas-Sahlin, andWeibull models by a non-linear regression equation. The antibacterial properties were evaluated using the disc diffusionmethod with respect to several wound gram-positive (Methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcusepidermidis, Staphylococcus aureus, and Klebsiella pneumoniae) and gram-negative bacteria (Pseudomonas aeruginosa,Salmonella typhimurium, and Proteus vulgaris). In general, the release behavior of Ciprofloxacin from PVP/Dex is controlledby diffusion in the delivery system.