Coumarin-Chalcone derivatives as promising antioxidant agents targeting ischemia/reperfusion injury through Nrf2 pathway activation.

Ischemic stroke remains a major global cause of mortality. Reperfusion therapy with thrombolysis paradoxically raises reactive oxygen species (ROS) and causes cerebral ischemia-reperfusion injury (CIRI). To address this challenge, antioxidants, which directly neutralize ROS or indirectly activate the KEAP1/Nrf2/ARE pathway, have emerged as promising strategies.

Synthesis, characterization, anti-proliferative, and apoptotic activity of a novel quinazoline-containing 1,2,3-triazole toward three human cancer cells.

A novel quinazoline-containing 1,2,3-triazole (4-TCPA) was synthesized to target VEGFR2 signaling for cancer treatment. Although current VEGFR2 inhibitors exhibit strong anticancer activity, their clinical use is limited due to severe side effects. Structural analysis of effective VEGFR2 inhibitors guided the design of 4-TCPA, ensuring the retention of Erlotinib's essential pharmacophoric features for optimal receptor binding.

Design, synthesis, and evaluation of triazolo[1,5-a]pyridines as novel and potent α‑glucosidase inhibitors.

α-Glucosidase is a key enzyme responsible for controlling the blood glucose, making a pivotal target in the treatment of type 2 diabetes mellitus. Present work introducestriazolo[1,5-a]pyridine as a novel, potent scaffold for α-glucosidase inhibition. A diverse scope of targeted compounds was prepared through an efficient, straightforward synthetic protocol.

Organic Peroxides in Transition-Metal-Free Cyclization and Coupling Reactions (C-C) via Oxidative Transformation.

Transition-metal-free transformations are recognized as green and sustainable methods for constructing carbon-carbon bonds in organic synthesis. This review describes the application of six organic peroxides, including -butyl hydroperoxide (TBHP), di--butyl peroxide (DTBP), -butyl peroxybenzoate (TBPB), benzoyl peroxide (BPO), dialauroyl peroxide (DLP), and diguyl peroxide (DCP), in C-C bond construction, highlighting selected examples and mechanisms of challenging transformations. Each section concludes with a detailed overview of suitable reagents for various coupling reactions and strengths and weaknesses of the reported works.

Psilocin alleviates acute itch in mice: possible involvement of 5-HT2A receptors and kynurenine pathway.

We aimed to investigate whether psilocin, the bioactive metabolite of the well-known psychedelic, psilocybin, may have antipruritic effects in mice by interfering with the kynurenine pathway and interacting with 5-HT2A receptors. Eight mice were randomly assigned to each of the study groups receiving either normal saline, compound 48/80, psilocin (0.3, 1, and 3 mg/kg), or psilocin (1 mg/kg) + 1-MT (0.

Psilocin, A Psychedelic Drug, Exerts Anticonvulsant Effects Against PTZ- and MES-Induced Seizures in Mice via 5-HT1A and CB1 Receptors: Involvement of Nitrergic, Opioidergic, and Kynurenine Pathways.

Epilepsy, a chronic neurological disorder affecting around 65 million people globally, is characterized by recurrent, unprovoked epileptic seizures. Psilocin, the active metabolite of psilocybin, a well-known psychedelic compound, has recently gained attention for its potential antidepressant and anxiolytic properties. This study aims to investigate the anticonvulsant effects of psilocin.

Lipoic acid scaffold applications in the design of multitarget-directed ligands against Alzheimer's disease.

Alzheimer's disease (AD) is becoming a fast-growing public health problem which can result in psychological problems as well as loss of speech, language, short-term memory, and motor coordination. Many medications were developed and produced to treat AD, however due to the complexity of the pathology involved in the illness, many of these medications often failed in clinical or preclinical studies. The main issue with the current anti-AD medications is their low efficacy since they use a single target.

Design, synthesis, and evaluation of novel substituted imidazo[1,2-c]quinazoline derivatives as potential α-glucosidase inhibitors with bioactivity and molecular docking insights.

α-Glucosidase inhibitors are important in the treatment of type 2 diabetes by regulating blood glucose levels and reducing carbohydrate absorption. The present study focuses on identifying new inhibitors bearing imidazo[1,2-c]quinazoline backbone through multi-step synthesis. The inhibitory potencies of the novel derivatives were tested against Saccharomyces cerevisiae α-glucosidase, revealing IC values ranging from 50.

Identification of furo[2,3-d]pyrimidin-4-ylsulfanyl-1,3,4-thiadiazole derivatives as novel FLT3-ITD inhibitors.

Given the significant prevalence of FLT3 receptor and its mutations in acute myeloid leukemia (AML) pathogenesis, we present a novel series of furo[2,3-d]pyrimidin-1,3,4-thiadiazole-urea derivatives, designed to exhibit FLT3-ITD inhibitory activity. These compounds demonstrated cytotoxicity in FLT3-ITD expressing AML cell lines MOLM-13 and MV4-11 in the nanomolar range, with significant selectivity over the K562 cell line. In-depth evaluations of example compound 49 revealed its efficacy in suppressing FLT3 phosphorylation and the downstream signaling molecules, including STAT5 and ERK1/2.

Liraglutide alleviated alpha-pyrrolidinovalerophenone (α-PVP) induced cognitive deficits in rats by modifying brain mitochondrial impairment.

The use of NPS compounds is increasing, and impairment in spatial learning and memory is a growing concern. Alpha-pyrrolidinovalerophenone (α-PVP) consumption, as a commonly used NPS, can impair spatial learning and memory via the brain mitochondrial dysfunction mechanism. Liraglutide isone of the most well-known Glucagon-Like Peptide 1 (GLP-1) agonists that is used as an anti-diabetic and anti-obesity drug.

Retraction: Synthesis and characterization of a supported Pd complex on volcanic pumice laminates textured by cellulose for facilitating Suzuki-Miyaura cross-coupling reactions.

[This retracts the article DOI: 10.1039/D0RA04521G.].

Synthesis, biological activities, and molecular docking studies of triazolo[4,3-b]triazine derivatives as a novel class of α-glucosidase and α-amylase inhibitors.

In diabetes mellitus, amylase and glucosidase enzymes are the primary triggers. The main function of these enzymes is to break macromolecules into simple sugar units, which directly affect blood sugar levels by increasing blood permeability. To overcome this metabolic effect, there is a need for a potent and effective inhibitor capable of suppressing the enzymatic conversion of sugar macromolecules into their smaller units.

Consumption of non-antibacterial drugs may have negative impact on colonization in the stomach.

Background: Nineteen non-antibacterials were examined to show that their consumption for treatment of other diseases may inhibit . Four antibiotics were used for comparison.

Materials And Methods: Agar dilution method was used to examine the susceptibility of 20  isolates to 4 antibiotics; metronidazole (MTZ), clarithromycin (CLR), amoxicillin (AMX), tetracycline (TET) and 19 non-antibacterials; proton pump inhibitors (PPIs), H-blockers, bismuth subsalicylate (BSS), antifungals, statins, acetaminophen (ACE), aspirin (ASA), B-vitamins (B-Vits; Vit B1, Vit B6 and Vit B and vitamin C (Vit C).

PEI-based functional materials: Fabrication techniques, properties, and biomedical applications.

Cationic polymers have recently attracted considerable interest as research breakthroughs for various industrial and biomedical applications. They are particularly interesting due to their highly positive charges, acceptable physicochemical properties, and ability to undergo further modifications, making them attractive candidates for biomedical applications. Polyethyleneimines (PEIs), as the most extensively utilized polymers, are one of the valuable and prominent classes of polycations.

Novel quinazolines bearing 1,3,4-thiadiazole-aryl urea derivative as anticancer agents: design, synthesis, molecular docking, DFT and bioactivity evaluations.

A novel series of 1-(5-((6-nitroquinazoline-4-yl)thio)-1,3,4-thiadiazol-2-yl)-3-phenylurea derivatives 8 were designed and synthesized to evaluate their cytotoxic potencies. The structures of these obtained compounds were thoroughly characterized by IR, H, and C NMR, MASS spectroscopy and elemental analysis methods. Additionally, their in vitro anticancer activities were investigated using the MTT assay against A549 (human lung cancer), MDA-MB231 (human triple-negative breast cancer), and MCF7 (human hormone-dependent breast cancer).

Synthesis and Biological Evaluation of 12-Aryl-11-hydroxy-5,6-dihydropyrrolo[2″,1″:3',4']pyrazino[1',2':1,5]pyrrolo[2,3-]pyridazine-8(9)-one Derivatives as Potential Cytotoxic Agents.

In the present paper, a facile and efficient synthetic procedure has been applied to obtain dihydrodipyrrolo[1,2-:2',1'-]pyrazine-2,3-dicarboxylates (-), which have subsequently gone through the cyclization in the presence of hydrazine hydrate to afford 12-aryl-11-hydroxy-5,6-dihydropyrrolo[2″,1″:3',4']pyrazino[1',2':1,5]pyrrolo[2,3-]pyridazine-8(9)-ones (-). The molecular structures of these novel compounds were extensively examined through the analysis of spectroscopic data in combination with X-ray crystallography techniques. Following that, the cytotoxic activities of all derivatives against three human cancer cell lines (Panc-1, PC3, and MDA-MB-231) were comprehensively evaluated alongside the assessment on normal human dermal fibroblast (HDF) cells using the MTT assay.

Imidazo[1,2-c]quinazolines as a novel and potent scaffold of α-glucosidase inhibitors: design, synthesis, biological evaluations, and in silico studies.

α-Glucosidase inhibition is an approved treatment for type 2 diabetes mellitus (T2DM). In an attempt to develop novel anti-α-glucosidase agents, two series of substituted imidazo[1,2-c]quinazolines, namely 6a-c and 11a-o, were synthesized using a simple, straightforward synthetic routes. These compounds were thoroughly characterized by IR, H and C NMR spectroscopy, as well as mass spectrometry and elemental analysis.

Imidazopyridine-based kinase inhibitors as potential anticancer agents: A review.

Considering the fundamental role of protein kinases in the mechanism of protein phosphorylation in critical cellular processes, their dysregulation, especially in cancers, has underscored their therapeutic relevance. Imidazopyridines represent versatile scaffolds found in abundant bioactive compounds. Given their structural features, imidazopyridines have possessed pivotal potency to interact with different protein kinases, inspiring researchers to carry out numerous structural variations.

Tannic acid-mediated synthesis of flower-like mesoporous MnO nanostructures as T-T dual-modal MRI contrast agents and dual-enzyme mimetic agents.

This study introduces a simple method for preparing a new generation of MnO nanomaterials (MNMs) using tannic acid as a template. Two shapes of MnO NMs, flower-like M1-MnO and near-spherical M2-MnO, were prepared and compared as dual-active nanozymes and contrast agents in magnetic resonance imaging (MRI). Various parameters, including the crystallinity, morphology, magnetic saturation (M), surface functionality, surface area, and porosity of the MNMs were investigated.

Quinazoline-based VEGFR-2 inhibitors as potential anti-angiogenic agents: A contemporary perspective of SAR and molecular docking studies.

Angiogenesis, the formation of new blood vessels from the existing vasculature, is pivotal in the migration, growth, and differentiation of endothelial cells in normal physiological conditions. In various types of tumour microenvironments, dysregulated angiogenesis plays a crucial role in supplying oxygen and nutrients to cancerous cells, leading to tumour size growth. VEGFR-2 tyrosine kinase has been extensively studied as a critical regulator of angiogenesis; thus, inhibition of VEGFR-2 has been widely used for cancer treatments in recent years.

Novel fluoroquinolones analogues bearing 4-(arylcarbamoyl)benzyl: design, synthesis, and antibacterial evaluation.

Bacterial resistance to fluoroquinolone has been increasing at an alarming rate worldwide. In an attempt to find more potent anti-bacterial agents, an efficient, straightforward protocol was performed to obtain a large substrate scope of novel ciprofloxacin and sarafloxacin analogues conjugated with 4-(arylcarbamoyl)benzyl 7a-ab. All prepared compounds were evaluated for their anti-bacterial activities against three gram-positive strains (Methicillin resistant staphylococcus aureus (MRSA), Staphylococcus aureus, and Enterococcus faecalis) as well as three gram-negative strains (Pseudomonas aeruginosa, Klebsiella pneumonia, and Escherichia coli) through three standard methods including broth microdilution, agar-disc diffusion, and agar-well diffusion assays.

Synthesis, α-Glucosidase inhibitory activity and docking studies of Novel Ethyl 1,2,3-triazol-4-ylmethylthio-5,6-diphenylpyridazine-4-carboxylate derivatives.

In this work, a novel series of pyridazine-triazole hybrid molecules were prepared and evaluated as inhibitors of rat intestinal α-glucosidase enzyme. Amongst all newly synthesized compounds, 10k showed good inhibition in the series with IC value of 1.7 µM which is 100 folds stronger than positive control, acarbose.

CuONPs/MWCNTs/carbon paste modified electrode for determination of tramadol: theoretical and experimental investigation.

A practical technique was applied to fabricate CuO nanostructures for use as the electrocatalyst. The green synthesis of cupric oxide nanoparticles (CuO NPs) via co-precipitation is described in this paper using an aqueous extract of Origanum majorana as both reductant and stabilizer, accompanied by characterization via XRD, SEM, and FTIR. The XRD pattern revealed no impurities, whereas SEM revealed low agglomerated spherical particles.

Alpha pyrrolidinovalerophenone (α-PVP) administration impairs spatial learning and memory in rats through brain mitochondrial dysfunction.

Novel psychoactive substances (NPS) consumption has increased in recent years, thus NPS-induced cognitive decline is a current source of concern. Alpha-pyrrolidinovalerophenone (α-PVP), as a member of NPS, is consumed throughout regions like Washington, D.C.