Background: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted on all derivatives. Molecular docking and ADMET analysis were performed on the final compounds, comparing them with standard drugs (ciprofloxacin and fluconazole). Results: The antimicrobial activity was assessed on two Gram-positive bacteria, Staphylococcus aureus and Bacillus licheniformis; two Gram-negative bacteria, Escherichia coli and Acinetobacter baumannii; and one fungus species, Candida albicans. Molecular docking has recorded higher docking scores for 3d and 3e compared to ciprofloxacin and fluconazole. The virtually active molecules showed an adequate drug-like profile and desired pharmacokinetic properties in the ADMET analysis. Conclusions: Most derivatives displayed significant antimicrobial activity, with compound 3e being the most active, followed by compound 3b. Molecular docking revealed higher scores for compound 3e compared to fluconazole and for compounds 3d and 3e compared to ciprofloxacin. ADMET analysis of compound 3e showed excellent absorption, consistent with its strong GIT absorption.
Background: This study evaluated the influence of different fiber formulations incorporation in resin composite on cuspal deflection (CD) of endodontically-treated teeth with mesio-occluso-distal (MOD) cavities. Materials and Methods: Thirty-two freshly extracted maxillary premolar teeth received MOD cavity preparation followed by endodontic treatment using single cone obturation technique, and divided into: Group I: direct composite resin only using a centripetal technique, Group II: direct composite resin with short fiber-reinforced composite (everX Flow), Group III: direct composite resin with leno wave ultra-high molecular weight polyethylene (LWUHMWPE) fibers placed on the cavity floor, and Group IV: direct composite resin with LWUHMWP
... Show MoreMyelosuppression is a serious disease that is related to the malfunction of blood cells production that leads to cytopenia which is the most serious hematologic toxicity of cancer chemotherapies including cyclophosphamide, which is a strong oxazaphosphorine [a nitrogen mustard alkylating agent] that can be used alone or combined with other chemotherapeutic agents for the treatment of different malignant diseases. It induces severe bone marrow suppression by damaging hematopoietic stem cells through the generation of oxidative stress. Fisetin is a hydrophobic polyphenolic compound with a wide range of pharmacological properties such as antioxidant, anti-inflammatory, antimicrobial, osteoprotective, antidiabetic, and anti-carcinogenic activit
... Show MoreMyelosuppression is a serious disease that is related to the malfunction of blood cells production that leads to cytopenia which is the most serious hematologic toxicity of cancer chemotherapies including cyclophosphamide, which is a strong oxazaphosphorine [a nitrogen mustard alkylating agent] that can be used alone or combined with other chemotherapeutic agents for the treatment of different malignant diseases. It induces severe bone marrow suppression by damaging hematopoietic stem cells through the generation of oxidative stress. Fisetin is a hydrophobic polyphenolic compound with a wide range of pharmacological properties such as antioxidant, anti-inflammatory, antimicrobial, osteoprotective, antidiabetic, and anti-carcinogenic
... Show MoreThis study aims to develop a thermosensitive mucoadhesive periodontal in situ gel of secnidazole for local release of drug for treatment of periodontitis, in order to increase the drug residence time and to increase patient compliance while lowering the side effects of the drug.
Cold method was used to prepare 30 formulas of secnidazole periodontal in situ gel, using different concentrations of thermosensitive polymers (poloxamer407 alone or in combination with poloxamer 188) and methyl cellulose (MC ) or hydroxypropyl methylcellulose (HPMC K4M )in different concentrations used as mucoadhesive polymer and the resultant formulations were subjected to several tests such as gelation temperature GT, appearance and pH value. The fo
... Show MoreEbastine (EBS) is a poorly water-soluble antihistaminic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS). The aim of the present work was to enhance the solubility, dissolution rate and micromeritic properties of the drug, by formulating it as spherical crystal agglomerates by Quasi Emulsion Solvent Diffusion (QESD) method.
Spherical crystal agglomerates (SCAs) were prepared in presence of three solvents dichloromethane (DCM), water and chloroform as a good solvent, poor solvent and bridging solvent respectively. Agglomeration of EBS involved the use of some hydrophilic polymers like polyethylene glycol 4000 (PEG 4000), polyvinyl pyrrolidine K30 (PVP K30), D-?-tocopheryl
... Show MoreThis paper presents studying the performance of three types of polyethersulfone (PES) membrane for the simultaneous removal of Co2+ ions, Cd2+ ions, and Pb2+ ions from binary and ternary aqueous solutions. Co2+ ions, Cd2+ ions, and Pb2+ ions with two different initial concentrations (e.g., 10 and 50 ppm) were selected as examples of heavy metals that contaminate the groundwater as a result of geological and human activities. This study investigated the effect of types of PES membrane and metal ions concentration on the separation process. For the binary aqueous solutions, the permeation flux of the PES2 membranes was higher for the separation process of solutions containing 50 ppm of Cd2+ ions and 10 ppm of Co2+ ions (24.7 L
... Show MoreContracting cancer typically induces a state of terror among the individuals who are affected. Exploring how glucose excess, estrogen excess, and anxiety work together to affect the speed at which breast cancer cells multiply and the immune system’s response model is necessary to conceive of ways to stop the spread of cancer. This paper proposes a mathematical model to investigate the impact of psychological panic, glucose excess, and estrogen excess on the interaction of cancer and immunity. The proposed model is precisely described. The focus of the model’s dynamic analysis is to identify the potential equilibrium locations. According to the analysis, it is possible to establish four equilibrium positions. The stability analys
... Show MoreAt thermal energies near stellar conditions, nuclear reactions are sensitive to resonance strengths of the nuclear reaction cross-section. In this paper, the resonance strengths of nuclear reaction were evaluated numerically by means of nuclear reaction rate calculations using a written Matlab code, at the energies of interest in stellar nuclear reactions. The results were compared with standard reaction before and after application of a statistical analyses, to select the best parameters that made theoretical results as close as possible to the standard values. Fitting was made for different temperature ranges up to 10 GK, 0.6 GK and 0.25 GK. The evaluated results showed that as the temperature range becomes narrower, more error is ad
... Show MoreAn attempt was made to evaluate the PV performance of one-axis daily tracking and fixed system for Baghdad, Iraq. Two experimental simulations were conducted on a PV module for that purpose. Measurements included incident solar radiation, load voltage and load current. The first experiment was carried out for six months of winter half of year to simulate the one-axis daily tracking. The azimuth angle was due south while the tilt angle was being set to optimum according to each day of simulation. The second experiment was done at one day to simulate the PV module of fixed angles. It is found that there is a significant power gain of 29.6% for the tracking system in respect to the fixed one. The one-axis daily tracking was much more effect
... Show MoreProstate cancer is an important and potentially fatal disease in humans. Both genetic and environmental risk factors are associated with increased risk of prostate cancer among Asian pop