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.
The aim of the present study is to formulate floating effervescent microsponge tablet of the narrow absorption window drug, Baclofen (BFN) for controlling drug release and thereby decrease the side effect of the drug. The microsponges of BFN were prepared by non-aqueous emulsion solvent diffusion method (oil in oil emulsion method). The effects of drug: polymer ratio, stirring time and type of Eudragit polymer on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selected microsponge formula was incorporated into the floating effervescent gastro-retentive tablet. The prepared fl
... Show MoreThe preferred route of drug administration is the oral route, but drugs with narrow absorption window in the gastrointestinal tract are still challenging. The ability to extend and monitor the gastric emptying time is a valuable tool for processes remaining in the stomach longer than other traditional dosage forms.
The purpose of this study was to formulate and evaluate gastroretentive superporous hydrogel (SPH) of carvedilol with view to improve its solubility and increase gastric residence time in order to get sustained release formulas via utilization of various kinds and concentrations of hydrophilic polymers then after, incorporate the best prepared formula into capsules.
Sixteenth formulae of SPH h
... Show MoreThe study was conducted at the fields of the Department of Horticulture and Landscape Gardening, College of Agriculture Engineering Sciences, University of Baghdad. During the spring 2017. All the recommended practices were followed during experimentation. The experimental material consisted four Genotype it is Batraa, Btera, Mosulle, and local selection. The experiment was applied in Randomized Complete Block Design (RCBD). The objectives of Study were to estimate the some genetic parameters and path coefficient for some traits Okra, The results of statistical analysis for these genotypes were highly significant differences for all traits except the traits number of leaves, the numbe
Sumatriptan(ST) is a selective agonist at serotonin 5-HTI receptors, as well as 5-HT1B/1D subtypes. It is effective for acute migraine attacks, but has a short half life (about 2 hours) and low oral bioavailability (15%). The purpose of this study was to develop and optimize nasal mucoadhesive in-situ gel(IG) of ST to enhance nasal residence time for migraine management. Cold method was used to prepare different formulas of ST nasal IG, using thermosensitive polymers (poloxamer 407 alone or with poloxamer 188) with a mucoadhesive polymer hyaluronic acid (HA) which were examined for gelation temperature and gelation time, pH, drug content, gel strength, spreadability, muc
... Show MoreMeloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.
The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers.
Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content, water so
... Show MoreAugust Wilson’s major concern is to communicate the African American cultural awareness; to establish a counter-culture based on self-confidence and assertiveness. He advocates an encouraging attitude to elevate the African Americans’ spiritual consciousness and to teach them how to sublimate their aims in life. He aspires to win the everlasting battle against racial discrimination, oppression, injustice, and identity confusion. Sublimation, as a defense mechanism, will be Wilson’s new ammunition to re-read and to re-interpret the psychic constitution of his people, to help them get out of their self-imposed fences and this is the core of Wilson’s new culture. Sublimation is the process in which the psyche directs the negative drive
... Show MoreSince its invention by the Ancient Romans and later developed during the mid-18th century, the concrete structure and finish, has been considered as the most powerful, practical, economic and constructional material that meets the building’s architectural and aesthetical requirements. By creating unique architectural forms, the pioneer architects used concrete widely to shape up their innovative designs and buildings.
The pre-mixed ultra-high performance concrete which manufactured by Lafarge.
The transparent concrete and cement that allow the light beams to pass through them, introduces remarkable well-lit architectural spaces within the same structural criteria. This product is a recyclable, sustainab
... Show MoreBackground: Toxin-producing Shiga Escherichia coli has been identified as a new foodborne pathogen that poses a significant health risk to humans. Shiga toxin-producing Escherichia coli can be found in raw cow milk and its derivatives. A small number of Escherichia coli strains that produce shiga toxin are pathogenic. Aim of study: The study aimed to see if there were any virulence genes in 50 milk samples that were typical of Entero-haemorrhagic E. coli and evaluate the Myrtus communis effects on these bacteria. Materials and Method: Milk samples were used to isolate E. coli bacteria (n= 27), biochemically analyzed, and genetically screened for virulence genes using a multiplex (PCR). The hydro-alcoholic extraction of Myrtus communis leave
... Show MoreThe current research aims to reveal the level of satisfaction of the mentors with the evaluation of their performance according to gender (male - female) and to formulate the predictive equation for the level of performance (dependent variable) from knowing the level of satisfaction with the evaluation (independent variable). (16 paragraphs) contains alternatives to the answer that measures the level of satisfaction (weak, medium, and high) (1,2,3), that is, with a hypothetical average of (32). It consisted of 100 educational counselors consisting of 45 males and 55 females, the results of the research concluded that the level of satisfaction with performance is below the mean when compared with the hypothetical average of the scale of s
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