Novel synthesis, ring transformation and anticancer activity of 1,3-thiazine, pyrimidine and triazolo[1,5-a]pyrimidine derivatives

Synthesis, heterocyclization and anticancer activity of a new series of heterocyclic compounds are described. Aminothiazine 1 was obtained from the base induced condensation of thiourea, benzaldehyde and ethyl cyanoacetate. The synthesis of N-phenyl amino pyrimidine derivative 2 was obtained as a result of reaction of aniline with compound 1. Compound 2 underwent ring opening and recyclization upon reaction with HCl or H2O2/ NaOH to afford the acid derivative 3 or oxazine 4, respectively. Thiazine 1 undergoes ring transformation upon the effect of NH2OH.HCl to produce pyrimidine derivative 5. Heterocyclization of compound 1 with thiosemicarbazide followed by oxidation with I2/AcOH afforded triazolopyrimidine 6 and 7, respectively. Alkylation of compound 1 was promoted by reaction of 1 with ethyl iodide to give alkylated thiazine 8 which in turn undergo ring transformation when subjected to reaction with hydrazine hydrate to give pyrazole derivative 9. Refluxing of amino-1,3-thiazine derivative 1 with ethyl bromoacetate in the presence of Et3N produce the alkylated pyrimidine product 10. Hydrazonolysis of 1,3-thiazine 1 with hydrazine or phenyhydrazine gave pyrimidine derivatives 11a,b, respectively. Compound 11b was cyclized with carbon disulfide or formaldehyde to produce triazolopyrimidines 12 and 13, respectively. Some of the new compounds were screened for anticancer activity and significant results were found for some compounds.               KEY WORDS: 1,3-Thiazine, Pyrimidine, Triazole, Pyrazole, Anticancer activity Bull. Chem. Soc. Ethiop. 2018, 32(3), 513-522.DOI: https://dx.doi.org/10.4314/bcse.v32i3.1

Simulation: Early Detection of Brain Vessels Stroke by Applying Electromagnetic Waves Non-Invasively

Introduction: Early recognition of stroke with its two types Ischemic and Hemorrhagic, is one of the most crucial research points, commonly used methods are CT- (computerized tomography), and MRI- (Magnetic resonance imaging). These techniques cause a delay in the detection of the condition, which causes permanent disability. The main reason behind the fatal consequences of stroke is the delay of detection. Therefore, this research paper aims to early detection of the type of stroke without delay until the appropriate diagnosis of each type is made, and then the appropriate treatment without delay. Method: Using a non-invasive and fast technique to determine the stroke type by wave, we simulate and design a vessel containing a liquid as a laminar flow with the same density and velocity of blood, and it was surrounded by a Homogenized multi-turn coil consisting of (n) turns to represent the magnetic field, using specific frequency (HZ) with Electrical field in coil current (A) to see the changing in magnetic flux density (MFD), Depending on the changes in MFD, the flow of blood in laminar flow can be affected by clotting (Ischemic) or Hemorrhagic (cutting) in our vessel designed. We have built three different scenarios to apply the technique which are: First: Normal Scenario (where the blood in vessel has no problem), second: clotting (ischemic, where the vessel blocked in specific three position) and Third: Cutting (Hemorrhagic, where the vessel cut in certain nine positions). Results: This paper presents-through our own design-the studying of applying the electromagnetic waves on blood inside the vessel to detect the stroke type in our three scenarios (normal, ischemic three positions or hemorrhagic nine positions), Studying the magnetic field and laminar flow. This study covered in three areas. First: coil geometry analysis, Second: stationary, and Third: frequency domain. through the changes in Magnetic Flux Density -MFD- waves. The results were promising and distinct for distinguishing between the three scenarios which are normal, ischemic (3 positions) and hemorrhagic (9 positions) the results of MFD are: 0.09 to 3.3*10^-3, 0.08 to 3.15*10^-4, 0.15 to 6.2*10^-3 respectively

Encapsulated polycaprolactone with triazole derivatives and selenium nanoparticles as promising antiproliferative and anticancer agents

Background and purpose Polycaprolactone nanocapsules incorporated with triazole derivatives in the presence and absence of selenium nanoparticles were prepared and evaluated as antiproliferative and anticancer agents. Polycaprolactone nanoparticles were prepared using the emulsion technique. Experimental approach The prepared capsules were characterized using FT-IR, TEM and DLS measurements. The synthesized triazolopyrimidine derivative in the presence and absence of selenium nanoparticles encapsulated in polycaprolactone was tested for its in vitro antiproliferative efficiency towards human breast cancer cell line (MCF7) and murine fibroblast normal cell line (BALB/3T3) in comparison to doxorubicin as a standard anticancer drug. Key results The results indicated that encapsulated polycaprolactone with selenium nanoparticles (SeNPs) and triazole-SeNPs were the most potent samples against the tested breast cancer cell line (MCF7). On the other hand, all compounds showed weak or moderate activities towards the tested murine fibroblast normal cell line (BALB/3T3). Conclusion As the safety index (SI) was higher than 1.0, it expanded the way for newly synthesized compounds to express antiproliferative efficacy against tumour cells. Hence, these compounds may be considered promising ones. However, they should be examined through further in-vivo and pharmacokinetic studies

Impact Factors on Subcontractor's Cash Flow Management

Objective: This study aims to define how to maintain and protect the subcontractor firms' cash flow from economic fluctuation through legally sustainable solutions. Methods/Analysis: We conducted a case study in the Eastern Delta Region of Egypt. A questionnaire containing a list of 22 impact factors on subcontractors' cash flow was distributed across multiple subcontractor firms with an 82% response rate. It was designed to explore the factors causing cash flow instability and analyze them using SPSS statistics. Findings: The study finds that inflation, late payments, non-compensation for late payments, poor subcontractor cash flow management, subcontractor firms' inclination to avoid disputes, material price fluctuation, and non-compensation terms, as well as suppliers rejection of payment delays, are the most critical factors of subcontractor cash flow problems. Novelty/Improvement:The study suggests adding three sub-articles to Article 57 in "Tender Law" as legally sustainable solutions to protect and maintain the firm's growth rate from inflation, late payment, and the inclination to avoid disputes. Also, the study recommends that the owner ensure that cash is available before procuring the general contractors, as stated in Egyptian Law 182 of 2018. This study will contribute to establishing a sustainable win-win relationship between subcontractors and general contractors. Doi: 10.28991/CEJ-SP2023-09-08 Full Text: PD

Preparation of Low Molecular Weight Natural Polymers by gamma-Radiation and Their Growth Promoting Effect on Zea Maize Plants

Preparation of oligosaccharides from chitosan and Na-alginate were done using ?-rays and H2O2 as oxidizing agent. Structural and molecular weight changes of such oligosaccharides were determined by GPC, FT-IR and UV-Vis. spectroscopy. FT-IR and UV-Vis. studies revealed that during radiation degradation process, the main polysaccharide chain structure was almost remained. The effects of spraying 100 ppm of oligochitosan or oligoalginate or both of them with different ratios on the growth of zea maize plants showed an enhancement of plant growth performance and the productivity at the same time suggesting their possible use in agriculture purposes as growth promoters for plants

Circulating dendritic cells in pediatric patients with nephrotic syndrome

Background: Dendritic cells (DCs) represent one of the most extensively studied topics in immunology, because of their central role in the induction and regulation of adaptive immunity, and because of their therapeutic potential for manipulating immune responses. Objectives: To evaluate circulating DC levels in pediatric patients with idiopathic nephrotic syndrome (NS) and its relation to disease activity in these patients. Methods: Fifteen nephrotic patients in relapse (proteinuria>40mg/m2/hour, hypoalbuminemia, and edema) before initiating steroid therapy (Group I), and another15 nephrotic patients in remission after withdrawal of steroid therapy (Group II) were compared to 15 age- and sex- matched healthy children. Besides clinical evaluation and routine laboratory investigations of nephrotic syndrome, circulating DCs were measured by flowcytometry. Results: Circulating DC count was lower in nephrotic patients in both proteinuria and remission groups [(48.89±13.52) and (64.64±7.69) X106/liter respectively] than in the control group (78.54±9.8) X106/liter with highly significant statistical difference (p < 0.001), and lower in proteinuria group than the remission group with highly significant statistical difference (p < 0.001). There was a positive correlation between DC count and serum albumin (moderate association) (p=0.002) and a negative correlation between DC count and urine protein /creatinine ratio (strong association) (p=0.001). Conclusion: Nephrotic syndrome was associated with decreased number of circulating DCs and the decrease was more apparent in patients with active disease. The positive correlation between DC counts and total protein, and serum albumin, and the negative correlation between DC count and urine protein/creatinine ratio point to the link between the decrease in DC count and the severity of the disease process.Keywords: Denderitic cells, nephrotic syndrome, immune deficiencyEgypt J Pediatr Allergy Immunol 2011;9(1):41-4

Quality of care of Egyptian asthmatic children: Clinicians adherence to asthma guidelines

<p>Abstract</p> <p>Background</p> <p>Despite the development and dissemination of guidelines for the diagnosis and management of asthma, a gap remains between current recommendations and actual practice.</p> <p>Objectives</p> <p>To assess the physicians attitude towards asthma guidelines and their adherence to its recommendations.</p> <p>Methods</p> <p>Three hundred and fifty two clinicians (101 General practitioners, 131 pediatric specialists, 35 pediatric consultants and 85 doctors did not report the qualification) engaged in direct childhood asthma care in Cairo, Egypt were subjected to a self-administered questionnaire with 35 questions of which most were multiple choices, aiming at assessment of three important aspects about the involved physicians; physician's knowledge, practice and attitude. 165 of the clinicians were working in governmental hospitals, 68 clinicians work in private clinics and 119 clinicians work in both.</p> <p>Results</p> <p>Agreement with asthma guidelines was present in 76.2% of the studied physicians, however those who not in agreement with the guidelines claimed that this was mainly due to patient factors, firstly the poor socioeconomic standard of the patient (18.1%) and secondly due to poor patient compliance (16%). Poor knowledge was found in 28.5%, poor practice was found in 43.6% and poor attitude was found in 14.4% of the studied physicians. There was positive highly significant correlation between qualification and knowledge, (p < 0.01), positive highly significant correlation between qualification and practice, (p < 0.01), and positive highly significant correlation between qualification and attitude, (p < 0.01).</p> <p>Conclusion</p> <p>The attitude of the studied physicians revealed agreement of their majority with the guidelines, while the disagreement was mainly explained by the poor socioeconomic standard of the patients. The degree of poor practice is more marked than that of poor knowledge or poor attitude reflecting resources limitations and applications obstacles in the physician's practice.</p

On modeling two immune effectors two strain antigen interaction

In this paper we consider the fractional order model with two immune effectors interacting with two strain antigen. The systems may explain the recurrence of some diseases e.g. tuberculosis (TB). The stability of equilibrium points are studied. Numerical solutions of this model are given. Using integer order system the system oscillates. Using fractional order system the system converges to a stable internal equilibrium. Ulam-Hyers stability of the system has been studied