Synthesis and radiolabelled evaluation of novel pyrimidine derivatives as dual α-amylase inhibitors and GIT-targeted molecular imaging probe.

This study successfully developed synthetic pathways for novel pyrimidine-based compounds for their potential anti-diabetic α-amylase inhibitory activity, aiming at potential antidiabetic applications. Molecular docking techniques showed that compounds 1, 6, and 8 showed the highest molecular docking binding affinity, followed by estimation. Compound 1 showed the strongest inhibitory amylase effect, in comparison to the reference drug acarbose.

A multifunctional Cu-Pyrazolone complex: green synthesis, radiolabeling, molecular docking, and tumor-targeted theranostic evaluation.

Theranostic agents that combine diagnostic imaging and targeted therapy are reshaping how we detect and treat cancer. In this work, we introduce a newly synthesized pyrazolone-based compound, designed with sustainability in mind using a green synthetic route. The ligand, 5-(2-hydroxyphenyl)-2,4-dichloro-3H-pyrazol-3-one, was structurally confirmed and efficiently radiolabeled with the copper isotopes ⁶⁴Cu and ⁶⁷Cu enabling both PET imaging and therapeutic functions.

DFT Investigations and Molecular Docking as Potent Inhibitors of SARS-CoV-2 Main Protease of Novel Pyrimidine Dione Derivatives.

The global outbreak of SARS-CoV-2 has emerged as a major public health crisis due to its rapid transmission and significant morbidity and mortality rates. In response, there is an urgent need to discover novel antiviral agents targeting key viral proteins. In this study, a new series of pyrimidine-2,4-dione derivatives was synthesized from barbituric acid and its thio analog, aiming to explore their potential inhibitory activity against the SARS-CoV-2 main protease (Mpro).

Dual α-amylase and α-glucosidase inhibition by 1,2,4-triazole derivatives for diabetes treatment.

The development of effective antidiabetic agents remains a critical challenge in diabetes management. In this study, we introduce novel 1,2,4-triazole-based derivatives designed as dual inhibitors of α-amylase and α-glucosidase, key enzymes in carbohydrate metabolism. Molecular docking identified six promising candidates, with compounds 4 and 10 showing the highest potency.

Gamma ray shielding capability of flexible silicone rubber composites reinforced with recycled CRT glasses.

With a focus on extending the horizons of combining electronic waste (e-waste) with different materials for creating efficient, affordable, eco-friendly, and sustainable radiation shielding composites, the present study investigates the radiation shielding performance of different composites made of silicon rubber and e-waste glass. Six samples were prepared by mixing different amounts of powdered cathode ray tube (CRT) glass (0-50%) with silicon rubber (100-50%). The linear attenuation coefficients (LAC's) of the prepared samples were experimentally measured using a high-purity germanium detector and varying energy gamma sources.

Benzimidazole chemistry in oncology: recent developments in synthesis, activity, and SAR analysis.

A six-membered benzene ring is fused with a five-membered imidazole ring at positions four and five, generating benzimidazole, the benzo derivative of imidazole and a bicyclic aromatic chemical compound. Benzimidazole is a significant pharmacophore in a variety of physiologically active heterocyclic compounds due to its distinctive characteristics and structural framework. Because benzimidazole is both aromatic and heterocyclic, it interacts with a range of biological targets metal ion interactions, π-π stacking, and hydrogen bonding.

Triphosgene/KF-mediated acyl fluoride synthesis fluoro(chloro)phosgene.

The transformation of carboxylic acids into acyl fluorides triphosgene-mediated deoxyfluorination utilizing inexpensive potassium fluoride (KF) has been achieved. This method affords a diverse range of acyl fluorides in high yields and exceptional purity. Analysis using F NMR spectroscopy reveals that fluorophosgene and chlorofluorophosgene, generated , serve as the reactive intermediates crucial to the conversion process.

Bio-computational modeling, POM analysis and molecular dynamic simulation for novel synthetic quinolone and benzo[d][1,3]oxazine candidates as antimicrobial inhibitors.

The current study offers a metal-free, direct, and successful synthesis technique for a new series of quinolinone and benzo[d][1,3]oxazine, along with an assessment of their biological activities. Heteroannulation of anthranilic acid with carbonyl-containing chemicals (aroyl pyruvate, ethyl acetoacetatete, maleic anhydride, and ethyl cyanoacetate) resulted in the desired quinolones and benzo[d][1,3]oxazines. This technique introduces a number of fundamental breakthroughs in organic synthesis, including metal-free catalysts, smart reaction conditions with column purification, and a wide functional scope.

Pharmacokinetic and molecular docking studies to pyrimidine drug using MnO nanoparticles to explore potential anti-Alzheimer activity.

Alzheimer disease (AD) is the cause of dementia and accounts for 60-80% cases. Tumor Necrosis Factor-alpha (TNF-α) is a multifunctional cytokine that provides resistance to infections, inflammation, and cancer. It developed as a prospective therapeutic target against multiple autoimmune and inflammatory disorders.

NBRM9, an extremophilic actinomycete producing extremozyme cellulase, using lignocellulosic agro-wastes and its biotechnological applications.

Actinomycetes are an attractive source of lignocellulose-degrading enzymes. The search for actinomycetes producing extremozyme cellulase using cheap lignocellulosic waste remains a priority goal of enzyme research. In this context, the extremophilic actinomycete NBRM9 showed promising cellulolytic activity in solid and liquid assays.

CuO nanoparticles for green synthesis of significant anti-Helicobacter pylori compounds with in silico studies.

Helicobacter pylori (H. pylori) is a universal health intimidation as mentioned by the World Health Organization. The primary causal agent linked to a number of illnesses, including inflammation and the development of stomach ulcers, is Helicobacter pylori.

Validation and Cultural Adaptation of the Parent Attitudes about Childhood Vaccines (PACV) Questionnaire in Arabic Language Widely Spoken in a Region with a High Prevalence of COVID-19 Vaccine Hesitancy.

The parents’ attitude toward vaccinating children and adolescents against coronavirus disease 2019 (COVID-19) remains inconsistent and needs further elucidation. The high rates of COVID-19 vaccine hesitancy in the Middle East and North Africa (MENA) region require intensive research to understand the determinants of this phenomenon. This study aimed to validate a version of the Parent Attitudes about Childhood Vaccines (PACV) tool in Arabic, the most widely spoken language in the MENA.

TiO nanoparticle as catalyst for an efficient green one-pot synthesis of 1H-3-Indolyl Derivatives as significant antiviral activity.

Titanium dioxide nanoparticles (TiO- NPs) are produced in large quantities for an extensive range of applications. They retain variable physicochemical properties, which influence their bioactivity. The condensation synthesis of 3-acetylindol, thiophene-2-carbaldehyde and malononitrile in the existence of TiO nanoparticle yields 2-amino-6-(1H-indol-3-yl)-4-(thiophen-2-yl)-4H-pyran-3-carbonitrile derivatives.

Silymarin inhibits the progression of Ehrlich solid tumor via targeting molecular pathways of cell death, proliferation, angiogenesis, and metastasis in female mice.

Background: Plant-derived phytochemicals have been reported to exert anticancer activity. This study investigated the antitumor role of silymarin (Silybum marianum) (SMN) and its molecular targets in Ehrlich solid tumor xenografts in vivo.

Methods And Results: Female Swiss albino mice were divided into three groups (of five animals each) that were engrafted with Ehrlich tumor (ET) cells with or without SMN treatment.

Combined Treatment of Adipose Derived-Mesenchymal Stem Cells and Pregabalin Is Superior to Monotherapy for the Treatment of Neuropathic Pain in Rats.

Aims: Neuropathic pain following nerve injury does not respond well to most available pharmacological remedies. We aimed to compare the outcome of the addition of adipose-derived mesenchymal stem cells (ADMSCs) to pregabalin for neuropathic pain treatment.

Methods: Adult female albino rats ( = 100) were randomized to receive traumatic sciatic nerve injury or sham.

Patterns of brain injuries associated with maxillofacial fractures and its fate in emergency Egyptian polytrauma patients.

Purpose: Maxillofacial injuries are commonly encountered in the practice of emergency medicine. More than 50% of patients with these injuries have multisystem trauma that requires coordinated management between emergency physicians and surgical specialists in oral and maxillofacial surgery, otolaryngology, plastic surgery, ophthalmology, and trauma surgery. The aim of this study is to identify the patterns of brain injuries associated with maxillofacial trauma and its outcome.