Synthesis, Glucosidase Inhibition, and In Silico Modeling Analysis of Highly Fluorinated 2-Imino-1,3-thiazolines in Search of Potent Antidiabetic Agents.

In the present work, 2-imino-1,3-thiazolines featuring highly fluorinated fragments were synthesized through a straightforward cyclization of diversely substituted thioureas with 2-bromo-1-(4-fluorophenyl)ethan-1-one. The target compounds were obtained in good yields, and structures were established by FTIR and 1H- and 13C NMR spectroscopic methods. The in vitro biological assay revealed that all the compounds significantly obstruct the α-glucosidase. Compound 6d (3-fluoro-N-(3-(2-fluorophenyl)-4-(4-fluorophenyl)thiazol-2(3H)-ylidene)benzamide) showed the highest antidiabetic potential with an IC50 value of 1.47 ± 0.05 µM. In addition, computational analysis revealed the binding energy of -11.1 kcal/mol for 6d which was lower than the positive standard, acarbose (-7.9 kcal/mol). Several intermolecular interactions between the active site residues and 6d highlight the significance of 2-imino-1,3-thiazoline core in attaining the potent efficacy and making these compounds a valuable pharmacophore in drug discovery.

Influence of Geometric Parameters on the Charging process of PCM in Semi-circular thermal storages for energy management.

The limitation of intermittent and irregular supply of the solar energy systems can be compensated through utilization of thermal energy storage systems. The design of an efficient latent heat thermal energy storage system plays a huge role in determining the overall performance. Therefore, this study aims to investigate the effect of geometric parameters such as thermal charger interspacing and inclination angle on the charging performance of a PCM (phase change material) inside a semi-circular enclosure with two charging sources (renewable heat sources). A numerical analysis is performed using the enthalpy-porosity method. The system performance is assessed in terms of dimensionless flow parameters such as Fourier number, Rayleigh number, and Stefan number. The study shows that the variation of Rayleigh number significantly influences the natural convection in the fluid zone of a PCM. An increase of Rayleigh number from 1e4 to 5e5 reduced the overall melting time by more than half. In addition, the thermal charger interspacing and inclination angle both showed considerable effect on the flow physics which can cause significant expedition/delay of the melting process.

Genomic and Therapeutic Analyses of Staphylococcus aureus Isolated from Cattle Reproductive Tract.

Staphylococcus aureus is emerging as a ubiquitous multidrug-resistant pathogen circulating among animals, humans, and their environment. The current study focused on molecular epidemiology and evidence-based treatment against S. aureus from bovine endometritis. For this study, n = 304 cattle were screened for endometritis using ultrasonography while presenting case history, and clinical signs were also considered. S. aureus was isolated from endometritis-positive uterine samples which were further put to molecular identification, phylogenetic analysis, susceptibility to antibiotics, and testing of novel drug combinations in both in vitro and field trials. The findings of the study revealed 78.20% of bovine endometritis samples positive for S. aureus, while nuc gene-based genotyping of S. aureus thermal nuclease (SA-1, SA-2, and SA-3) showed close relatedness with S. aureus thermal nuclease of Bos taurus. Drug combinations showed 5.00 to 188.88% rise in zones of inhibitions (ZOI) for drugs used in combination compared to the drugs used alone. Gentamicin in combination with amoxicillin and enrofloxacin with metronidazol showed synergistic interactions in an in vitro trial. Co-amoxiclav with gentamicin, gentamicin with enrofloxacin, and metronidazole with enrofloxacin showed 100%, 80%, and 60% efficacy in treating clinical cases in field trials, respectively. As a result, the study came to the conclusion the higher prevalence of endometritis-based S. aureus, genetic host shifts, narrow options for single drugs, and need for novel drug combinations to treat clinical cases.

Divergent Analyses of Genetic Relatedness and Evidence-Based Assessment of Therapeutics of Staphylococcus aureus from Semi-intensive Dairy Systems.

Use of antibiotics without following standard guidelines is routine practice in developing countries which is giving rise to genetic divergence and increased drug resistance. The current study analyzed genetic divergence and drug resistance by S. aureus and therapeutic efficacy of novel antibiotic combinations. The study revealed that 42.30% (minimum 20%-maximum 70%) of milk samples are positive for S. aureus. Study also revealed seven SNPs in the S. aureus nuc gene (c.53A>G, c.61A>G, c.73T>C, c.93C>A, c.217C>T, c.280T>C, and c.331T>A). Local isolates Staph-2 and Staph-3 were closely related to Bos taurus nuc gene (bovine S. aureus), while Staph-1 was closely related to Homo sapiens (human S. aureus) indicating shifting of host. Change of two amino acids and staphylococcal nuclease conserved domain was observed in all local isolates of S. aureus. The isoelectric points predicted by protParam of Staph-1, Staph-2, and Staph-3 proteins were 9.30, 9.20, and 9.20, respectively. The antibiotic susceptibility profile of S. aureus presented highest resistance against penicillin (46.67%) and glycopeptide (43.33%). When a single antibiotic regimen was adopted in a field trial, the highest efficacy was reported in the case of oxytetracycline (80%) while lowest was presented by azithromycin. Among antibiotics' combined regimen, the highest efficacy (80%) was presented by gentamicin with oxytetracycline: cefotaxime with vancomycin; and ciprofloxacin with vancomycin. The current study concluded rising percentages of S. aureus from dairy milk, proofs of genetic host shifts, and altered responses of in on field therapeutics.

Pathological insights into camel mastitis.

Camel is a multipurpose animal bred to produce milk, meat, and transport and serves as a financial reserve for pastoralists by playing an important role in social prestige and prosperity. Camel milk is a good substitute for human milk because of its exceptional nutritional properties. Udder infections are considered one of the main limitations to camel farming. In recent decades, the disease has been reported by numerous camel-producing countries in Africa and Asia, such as Egypt, Somalia, Sudan, Kenya, Saudi Arabia, and Iraq. The current review provides an overview of the forms of camel mastitis, which can be clinical mastitis characterized by hardening and swelling of the breast, pain on palpation, and visible changes in the colour and texture of the milk or subclinical mastitis refers to the presence of inflammation with no obvious signs and it can be detected by indirect tests such as the California mastitis test (CMT), somatic cell count (SCC), and microbiological examination. Major pathogens of camel mastitis are Staphylococcus aureus, Streptococcus agalactiae, Escherichia coli, and Corynebacterium bovis. Regarding the risk factors for camel mastitis, this study provides an overview of the most important risk factors such as severe tick infestation, teat injuries, hygienic milking protocols, and physiological disorders causing mastitis. The use of indirect tests and bacteriological studies as diagnostic tools and their values for detecting camel mastitis will also be reviewed. Based on the above, further epidemiological studies on camel mastitis are needed to have solid scientific data on disease transmission, pathogen characterization, other possible risk factors or diagnostic methods, and the impact of the disease on public health. Proper control strategies should be adopted through early diagnosis, treatment and by avoiding potential risk factors to get good quality milk from camels.

Evidence-Based Tracking of MDR E. coli from Bovine Endometritis and Its Elimination by Effective Novel Therapeutics.

Antibiotic-resistant bacteria have become the predominant etiology of endometritis and thus require effective treatment approaches. We used ultrasonography coupled with clinical signs and presented complaints of reproductive issues to investigate the epidemiology, phylogenetic analysis, antimicrobial resistance, and development of novel therapeutics against Escherichia coli isolated from endometritis in bovine (n = 304 from 10 commercial dairy farms). The prevalence of bovine endometritis in this study was 43.75%, while among these, 72.18% samples were positive for E. coli. Nucleotide analysis performed through BLAST and MEGAX showed 98% similarity to the nucleotide sequence of the reference E. coli strain (accession number CP067311.1). The disk diffusion assay revealed pathogen resistance to most antibiotics. Pattern of MIC order of resistance was as follows: enrofloxacin < gentamicin < co-amoxiclav < streptomycin < amoxicillin < metronidazole < oxytetracycline. Field trials revealed the highest recovery rate (in terms of clearance of endometritis and establishment of pregnancy) in case of gentamicin + enrofloxacin (100%) and gentamicin alone (100%), followed by co-amoxiclav + gentamicin (84.61%), oxytetracycline alone (78.57%), and metronidazole + enrofloxacin (33.33%). Hence, the current study reported a higher prevalence of multidrug-resistant E. coli showing considerable similarity with reference strain, and finally, the effective response of novel antibiotics to treat cases.

Homogeneous and Multiphase Analysis of Nanofluids Containing Nonspherical MWCNT and GNP Nanoparticles Considering the Influence of Interfacial Layering.

The practical implication of nanofluids is essentially dependent on their accurate modelling, particularly in comparison with the high cost of experimental investigations, yet the accuracy of different computational approaches to simulate nanofluids remains controversial to this day. Therefore, the present study is aimed at analysing the homogenous, multiphase Eulerian-Eulerian (volume of fluid, mixture, Eulerian) and Lagrangian-Eulerian approximation of nanofluids containing nonspherical nanoparticles. The heat transfer and pressure drop characteristics of the multiwalled carbon nanotubes (MWCNT)-based and multiwalled carbon nanotubes/graphene nanoplatelets (MWCNT/GNP)-based nanofluids are computed by incorporating the influence of several physical mechanisms, including interfacial nanolayering. The accuracy of tested computational approaches is evaluated by considering particle concentration and Reynolds number ranges of 0.075-0.25 wt% and 200-470, respectively. The results demonstrate that for all nanofluid combinations and operational conditions, the Lagrangian-Eulerian approximation provides the most accurate convective heat transfer coefficient values with a maximum deviation of 5.34% for 0.25 wt% of MWCNT-water nanofluid at the largest Reynolds number, while single-phase and Eulerian-Eulerian multiphase models accurately estimate the thermal fields of the diluted nanofluids at low Reynolds numbers, but overestimate the results for denser nanofluids at high Reynolds numbers.