The present article focuses on the synthesis and biological evaluation of a novel anthranilic acid hybrid its diamides as antispasmodics. Methods: Due to predicted in silico methods spasmolytic activity, we synthesized molecule 2-(3-chlorophenyl)ethylamine. obtained was then applied acylation with different acyl chlorides. Using analysis, pharmacodynamic profiles compounds were predicted. A thorough conducted assessing their vitro antimicrobial, cytotoxic, anti-inflammatory ex vivo activity....

Anticoagulants prevent the blood from developing coagulation process, which is primary cause of death in thromboembolic illnesses. Phenindione (PID) a well-known anticoagulant that rarely employed because it totally prevents coagulation, can be life-threatening complication. The goal current study to synthesize drug-loaded Ag NPs slow down process. Methods: A rapid synthesis and stabilization silver nanoparticles as drug-delivery systems for phenindione were applied first time. Results:...

Background/Objectives: This study is an attempt to reveal the potential of two types interpenetrating polymer network (IPN) hydrogels based on poly(2-hydroxyethyl methacrylate) (PHEMA) and poly(N,N-dimethylacrylamide) (PDMAM). These IPNs were evaluated for their dermal delivery hydrophobic drug dexamethasone (DEX). Methods: The analyzed rheological behavior, swelling characteristics, drug-loading capacity with DEX. Drug release profiles studied in Franz diffusion cells PBS media. Finally,...

Metallosupramolecular cages and capsules have gained increasing popularity as both molecular containers anticancer agents. For successful combination of these properties a thorough analysis the effect guest encapsulation on host's cytotoxic is highly required. Here we report cytotoxicity modulation Pt(ii) Pd(ii)-linked M2L4 coordination upon molecules such pyrene caffeine. The activity against various human cancer cells (HT-29, T-24, HL-60 its resistant counterparts HL-60/Dox HL-60/CDDP)...

The current study describes the elaboration of a hybrid drug delivery platform for an intravesical application based on curcumin/gentamicin sulfate simultaneously loaded niosomes incorporated into thermosensitive in situ gels. Series were elaborated via thin film hydration method, evaluating impact non-ionic surfactants', cholesterol's, and curcumin's concentration. formulation composed equimolar ratio Span 60, Tween 30 mol% cholesterol was selected as optimal composition, due to high...

Fifteen 4-methyl-1,2,3-thiadiazole-based hydrazone derivatives 3a–d and sulfonyl hydrazones 5a–k were synthesized. They characterized by 1H-NMR, 13C NMR, HRMS. Mycobacterium tuberculosis strain H37Rv was used to assess their antimycobacterial activity. All compounds demonstrated significant minimum inhibitory concentrations (MIC) from 0.07 0.32 µM, comparable those of isoniazid. The cytotoxicity evaluated using the standard MTT-dye reduction test against human embryonic kidney cells HEK-293T...

Alzheimer's disease (AD) is considered a complex neurodegenerative condition which warrants the development of multitargeted drugs to tackle key pathogenetic mechanisms disease. In this study, two novel series melatonin- and donepezil-based hybrid molecules with hydrazone (3a-r) or sulfonyl (5a-l) fragments were designed, synthesized, evaluated as multifunctional ligands against AD-related mechanisms. Two lead compounds (3c 3d) exhibited well-balanced profile, demonstrating intriguing...

The metabolic syndrome and its associated co-morbidities have been recognized as predisposing risk factors for the development of metabolic-associated fatty liver disease (MAFLD). present study reports on beneficial effect

Dimethoxy derivatives of salicylaldehyde benzoylhydrazone containing a methoxy group on both aromatic rings were designed and synthesized. The compounds obtained in high yields, their structures confirmed by elemental analysis various spectral techniques. In vitro evaluation dimethoxy hydrazones demonstrated potent activity against the leukemic cell lines at low micro- nanomolar concentrations. Remarkably, two analogs showed exceptional antileukemic selectivity, with no toxicity observed...

Aripiprazole (ARZ) is an atypical antipsychotic drug used to treat a variety of mood and psychotic disorders, such as schizophrenia, bipolar disorder, major depressive autism, Tourette's syndrome. Although ARZ offers significant therapeutic benefits, its poor solubility in water requires the development delivery systems aimed at improving bioavailability drug. In this work, cryogels based on two natural products-agar β-cyclodextrin (CD)-were developed evaluated system for ARZ. The were...

Irritable bowel syndrome (IBS) is a functional gastroenterological disorder with complex pathogenesis and multifaceted therapy approaches, aimed at alleviating clinical symptoms improving the life quality of patients. Its treatment includes dietary changes drugs from various pharmacological groups such as antidiarrheals, anticholinergics, serotonin receptor antagonists, targeting chloride ion channels, etc. The present article focused on synthesis biological evaluation some mebeverine...

Ultra-high-performance liquid chromatography coupled to Orbitrap high-resolution mass spectrometry (UHPLC-HRMS) was recently employed in many fields obtain a rapid characterization of plant extracts. Kigelia africana (family Bignoniaceae) is quintessential African herbal medicinal with immense indigenous and non-medicinal applications. The aim the present research an in-depth metabolite profiling K. stem bark extract using UHPLC-HRMS conduct preliminary screening its anticancer activity...

Piperine amide analogs are synthesized by replacement of the piperidine moiety with different types cyclic amines, including adamantyl and monoterpene‐derived fragments. The compounds screened for activity against Mycobacterium tuberculosis H37Rv. most potent 1‐adamantyl hybrids, which combine nanomolar antimycobacterial low cytotoxicity human cells. presence quaternary carbon atom as main structural requirement anti‐ TB is pointed out a QSAR study. promising compound...

Aripiprazole (ARZ) is a medication used for the treatment of various diseases such as schizophrenia, bipolar disorder, major depressive autism, and Tourette’s syndrome. Despite its therapeutic benefits, ARZ characterized by poor water solubility which provoked development delivery systems in order to enhance solubility. In present work, nanoscale drug system based on N,N-dimethylacrylamide (DMAA) β-cyclodextrin triacrylate (β-CD-Ac3) potential aripiprazole vehicles was developed. The...

A plethora of pathophysiological events have been shown to play a synergistic role in neurodegeneration, revealing multiple potential targets for the pharmacological modulation Alzheimer's disease (AD). In continuation our previous work on new indole- and/or donepezil-based hybrids as neuroprotective agents, present study reports beneficial effects lead compounds series key pathognomonic features AD both cellular and vivo models. An enzyme-linked immunosorbent assay (ELISA) was used evaluate...

1H-benzimidazol-2-yl hydrazones with varying hydroxy and methoxy phenyl moieties were designed. Their effect on tubulin polymerization was evaluated in vitro porcine tubulin. The compounds elongated the nucleation phase slowed down comparably to nocodazole. possible binding modes of explored by molecular docking at colchicine site. anticancer activity against human malignant cell lines MCF-7 AR-230, as well normal fibroblast cells 3T3 CCL-1. demonstrated a marked antineoplastic low...

Breast cancer (BC) is the second leading cause of death in women, with more than 600,000 deaths annually. Despite progress that has been made early diagnosis and treatment this disease, there still a significant need for effective drugs fewer side effects. In present study, we derive QSAR models good predictive ability based on data from literature reveal relationships between chemical structures set arylsulfonylhydrazones their anticancer activity human ER+ breast adenocarcinoma...

In the last decade need of plant-derived cytotoxic compounds exceeds possibilities for obtaining them from naturally grown sources. vitro plant biotechnology offers a unique and often invaluable alternative production complex biologically active substances without harming flora. Astragalus glycyphyllos L. (Fabaceae) is native to Bulgaria that has been reported contain triterpenoid saponins flavonoids. It used in folk medicine as an antihypertensive, diuretic, anti-inflammatory, anti-tumour,...

Although no effective treatment for the Alzheimer's disease currently exist, some drugs acting as Acetylcholinesterase inhibitors, like galanthamine have positively affected such patients. β- and/or γ-secretase inhibitors are another type of potential drugs. Here we report synthesis new peptide-galanthamine derivatives, with expected inhibitory activity against both and β-secretase.The aim this work is obtaining peptide derivatives decreased toxicity compared to galanthamine.Syntheses were...

Oxidative stress is a common phenomenon of many liver disorders; it both affects patient survival and directly influences the applicability, effectiveness, toxicity drugs. In pursuit reliable natural remedies for hepatoprotection, this study reports on complete phytochemical characterization, antioxidant, hepatoprotective activities Prenanthes purpurea methanol-aqueous extract in an vitro model diclofenac-induced injury (DILI). An ultra high-performance liquid chromatography-high-resolution...

Differences in pH between the tumour interstitium and healthy tissues can be used to induce conformational changes nanocarrier structure, thereby triggering drug release at desired site. In present study, novel pH-responsive nanocarriers were developed by modifying conventional niosomes with hexadecyl-poly(acrylic acid)n copolymers (HD-PAAn). Niosomal vesicles prepared thin film hydration method using Span 60, 60/Tween 60 cholesterol as main constituents, HD-PAA modifiers of different...