Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl) amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones(5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones wassecerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds(5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.
Abstract
The purpose of our study was to develop Dabigatran Etexilate loaded nanostructured lipid carriers (DE-NLCs) using Glyceryl monostearate and Oleic acid as lipid matrix, and to estimate the potential of the developed delivery system to improve oral absorption of low bioavailability drug, different Oleic acid ratios effect on particle size, zeta potential, entrapment efficiency and loading capacity were studied, the optimized DE-NLCs shows a particle size within the nanorange, the zeta potential (ZP) was 33.81±0.73mV with drug entrapment efficiency (EE%) of 92.42±2.31% and a loading capacity (DL%) of 7.69±0.17%. about 92% of drug was released in 24hr in a controlled manner, the ex-vivo intestinal p
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Azo-ligand-(HL) ([4- ((2-hydroxyquinolin-3-yl) diazenyl) -N- (5-methylisoxazol-3yl) benzenesulfonamide]), (2- hydroxy quinolin derivative),reacts with the next metal ions (Cr (III), Fe (III),Co (II) and Cu(II)) forming stable complexes with unique geometries such as(tetrahedral for bothCo (II) and Cu (II), octahedral for both Cr (III) and Fe (III)). The creation of such complexes was detected by employing spectroscopic means involving ultraviolet-visible which proved the obtained geometries, Fourier transfer proved the involvement of coordinated water molecule in all complexes besides the pyrolysis (TGA & DSC) studies proved the coordination of water residues with metal ions inside the coordination sphere as well as chlorine atoms. Moreover
... Show MoreEighty five samples were taken from patients suffering from pneumonia. Seventy-eight isolates were diagnosed as following: Staphylococcus aureus (23), klebsiella pneumoniae (29), Streptococcus pneumoniae (15), Serratia sp. (4), Haemophilus influenzae (4) and Pseudomonas aeruginosa (3). The clinical isolates were tested for antibiotics sensitivity. They appeared highly resistance to penicillin G and Ampicillin at percentage 89.7 and 84.6% respectly while the results showed highly sensitivity to streptomycin at percentege of (12.8%). To study the antibacterial activity of Alium sativum, Eucalyptus microtheca leaves and Cydonia oblonga seeds extracts, five multi resistant strains were used by using agar well diffusion and disk methods at c
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Background In recent years, there has been a notable increase in the level of attention devoted to exploring capabilities of nanoparticles, specifically gold nanoparticles AuNPs, within context of modern times. AuNPs possess distinct biophysical properties, as a novel avenue as an antibacterial agent targeting Streptococcus Mutans and Candida Albicans. The aim of this study to create a nano-platform that has the potential to be environmentally sustainable, in addition to exhibiting exceptional antimicrobial properties against Streptococcus Mutans as well as Candida Albicans. Methods this study involved utilization of
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Background and Aim: The aryl hydrocarbon receptor (AhR) plays a pivotal role in spermatogenesis through its regulatory functions in redox balance and gene expression. This study aimed to investigate the effects of resveratrol (RES), a polyphenolic AhR modulator, and CH223191, a selective AhR antagonist, on male reproductive function in rats by assessing sperm quality, oxidative stress, testicular histopathology, and AhR gene expression. Materials and Methods: Forty adult male rats were randomly divided into four groups: (i) Control, (ii) dimethyl sulfoxide (vehicle), (iii) RES (100 mg/kg i.p., twice weekly), and (iv) AhR⁻ (CH223191, 10 mg/kg i.p., twice weekly), treated for 60 days. Post-treatment, sperm motility, survival, viabi
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A theoretical and protection study was conducted of the corrosion behavior of carbon steel surface with different concentrations of the derivative (Quinolin-2-one), namly (1-Amino-4,7-dimethyl-6-nitro-1H-quinolin-2-one (ADNQ2O)). Theoretically, Density Functional Theory (DFT) of B3LYP/ 6-311++G (2d, 2p) level was used to calculate the optimized geometry, physical properties and chemical inhibition parameters, with the local reactivity to predict both the reactive centers and to locate the possible sites of nucleophilic and electrophilic attacks, in vacuum, and in two solvents (DMSO and H2O), all at the equilibrium geometry. Experimentally, the inhibition efficiencies (%IE) in the saline solution (of 3.5%) NaCl were studied using potentiomet
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Background: Male infertility is a global concern and it tends to increase due to miscellaneous factors, such as environmental toxins and genetic and lifestyle choices. The aryl hydrocarbon receptor (AHR) has recently attracted attention due to its involvement in male infertility mechanisms and impact on sperm production and function. AHR, a versatile receptor expressed in various tissues, including the testes, regulates the genes involved in spermatogenesis. AHR activation is associated with cell cycle regulation and chromatin condensation during spermatogenesis. Objectives: This study aimed to investigate the influence of AHR activation on blood-testis barrier (BTB) integrity, focusing on the role of tight junction protein-1 (TJP1)
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Secure storage of confidential medical information is critical to healthcare organizations seeking to protect patient's privacy and comply with regulatory requirements. This paper presents a new scheme for secure storage of medical data using Chaskey cryptography and blockchain technology. The system uses Chaskey encryption to ensure integrity and confidentiality of medical data, blockchain technology to provide a scalable and decentralized storage solution. The system also uses Bflow segmentation and vertical segmentation technologies to enhance scalability and manage the stored data. In addition, the system uses smart contracts to enforce access control policies and other security measures. The description of the system detailing and p
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The paper aims to propose Teaching Learning based Optimization (TLBO) algorithm to solve 3-D packing problem in containers. The objective which can be presented in a mathematical model is optimizing the space usage in a container. Besides the interaction effect between students and teacher, this algorithm also observes the learning process between students in the classroom which does not need any control parameters. Thus, TLBO provides the teachers phase and students phase as its main updating process to find the best solution. More precisely, to validate the algorithm effectiveness, it was implemented in three sample cases. There was small data which had 5 size-types of items with 12 units, medium data which had 10 size-types of items w
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