Key Elements Involved in Alzheimer's Disease Progression.

Alzheimer's disease (AD) is a neurodegenerative disease associated with memory loss and a decline in cognitive behavior. It is a progressive brain disorder where an individual's intelligence and reasoning capabilities are highly affected. The ability to think and process any idea is impaired, which is quite common in elders aged above 60 years.

Multifactorial Evaluation of Honey from Pakistan: Essential Minerals, Antioxidant Potential, and Toxic Metal Contamination with Relevance to Human Health Risk.

Honey is prized for its nutritional and healing properties, but its quality can be affected by contamination with toxic elements. This study evaluates the nutritional value and health risks of fifteen honey samples from different agro-climatic regions of Pakistan. Physicochemical properties such as color, pH, electrical conductivity, moisture, ash, and solids content were within acceptable ranges.

Development of novel cyclopropyl tethered iminothiazolidinone-isatin hybrids as effective multi target intestinal alkaline phosphatase, urease and α-glucosidase inhibitors.

In the pursuit of potent enzyme inhibitors to combat metabolic and microbial diseases, here we report the rational design and synthesis of novel cyclopropyl-tethered 2-iminothiazolidin-4-one-isatin hybrids (7a-k), aimed at overcoming limitations of current therapeutics in terms of potency, selectivity, and safety. The structures were confirmed through spectroscopy and compounds were assessed for inhibitory potential against α-glucosidase, urease, and Intestinal Alkaline phosphatase (IALP). Notably, compound (7d) featuring n-heptyl chain exhibited the highest potency against IALP, with an IC₅₀ value of 55.

Evaluation of anti-arthritic and anti-inflammatory potential of Ajugarin-I from Ajuga Bracteosa wall ex. Benth against Freund's complete adjuvant induced arthritis.

Rheumatoid arthritis (RA) is a prolonged autoimmune disease that targets the lining of small joints, causing inflammation and destruction of bone and cartilage. Anti-inflammatory drugs are available but offer short-term relief with adverse side effects. The present research was planned to study the in-vivo antiarthritic potential of ajugarin-I, sequestered from the Ajuga bracteosa.

Correction: Novel pyrimidine linked acyl thiourea derivatives as potent α-amylase and proteinase K inhibitors: design, synthesis, molecular docking and ADME studies.

[This corrects the article DOI: 10.1039/D4RA05799F.].

Unveiling the cyclopropyl appended acyl thiourea derivatives as antimicrobial, α-amylase and proteinase K inhibitors: Design, synthesis, biological evaluation, molecular docking, DFT and ADMET studies.

Acyl thiourea scaffolds are frequently employed in drug development to discern unique and essential therapies for the eradication of the most challenging diseases. Hence, we developed a library of novel cyclopropyl incorporating acyl thiourea derivatives (4a-j) and evaluated their antimicrobial, α-amylase, and proteinase K inhibition potential. Compound (4h) (4-methoxy) demonstrated the strongest α-amylase inhibition (IC = 1.

Newly synthesized sulfonamide derivatives explored for DNA binding, enzyme inhibitory, and cytotoxicity activities: a mixed computational and experimental analyses.

The current research work reports the synthesis of three 4-((3-arylthiazolo[3,4-]isoxazol-5-yl)amino)benzene sulfonamide derivatives with a thaizaole(3,4-)isoxazole-based fused ring heterocyclic system. The synthesized and characterized derivatives, namely, 4-(3-(2-hydroxy-3-methoxyphenyl)thiazolo[3,4-]soxazole-5-ylamino)benzenesulfonamide (YM-1), 4-(3-(4-chlorophenyl)isoxazolo[3,4-]thiazol-5-ylamino)benzenesulfonamide (YM-2), and 4-(3-(3-hydroxyphenyl)isoxazolo[3,4-]thiazol-5-ylamino)benzenesulfonamide (YM-3) were further explored for their binding interactions with DNA and enzymes (urease and carbonic anhydrase). Cytotoxicity of these derivatives for both healthy (HEK-293) and cancerous (MG-U87) cells was determined by MTT analysis.

Novel pyrimidine linked acyl thiourea derivatives as potent α-amylase and proteinase K inhibitors: design, synthesis, molecular docking and ADME studies.

To discover promising therapeutic agents, novel diaryl pyrimidine linked acyl thiourea derivatives (6a-j) were designed and synthesized straightforward and multistep synthesis. The structure of these derivatives (6a-j) was confirmed by FTIR, H, and C NMR spectroscopic techniques. The biological screening of these compounds was carried out to assess their bacterial, α-amylase, and proteinase K inhibition potential.

Exploring Acyl Thiotriazinoindole Based Pharmacophores: Design, Synthesis, and SAR Studies with Molecular Docking and Biological Activity Profiling against Urease, α-amylase, α-glucosidase, Antimicrobial, and Antioxidant Targets.

A diminutive chemical library of acyl thiotriazinoindole (ATTI) based bioactive scaffolds was synthesized, instigated by taking the economical starting material Isatin, through a series of five steps. Isatin was first nitrated followed by the attachment of pentyl moiety via nucleophilic substitution reaction. The obtained compound was reacted with thiosemicarbazide to obtain thiosemicarbazone derivative, which was eventually cyclized using basic conditions in water as solvent.

Kappa-carrageenan and sodium alginate-based pH-responsive hydrogels for controlled release of methotrexate.

Despite remarkable progress in medical sciences, modern man is still fighting the battle against cancer. In 2022, only in the USA, 640 000 deaths and 2 370 000 patients were reported because of cancer. Chemotherapy is the most widely used for cancer treatments.

Cloning of maize chitinase 1 gene and its expression in genetically transformed rice to confer resistance against rice blast caused by Pyricularia oryzae.

Fungal pathogens are one of the major reasons for biotic stress on rice (Oryza sativa L.), causing severe productivity losses every year. Breeding for host resistance is a mainstay of rice disease management, but conventional development of commercial resistant varieties is often slow.

Novel pyrazoline linked acyl thiourea pharmacophores as antimicrobial, urease, amylase and α-glucosidase inhibitors: design, synthesis, SAR and molecular docking studies.

In the present work, a small library of novel pyrazolinyl-acyl thiourea (5a-j) was designed and synthesized through a multistep sequence and the synthesized compounds were screened for their antifungal, antibacterial and antioxidant activities as well as urease, amylase and α-glucosidase inhibitory activities. The synthesized series (5a-o) was characterized using a combination of spectroscopic techniques, including FT-IR, H NMR and C NMR. All compounds (5a-j) were found to have significant potency against urease, α-glucosidase, α-amylase, and DPPH.

Bioassays guided isolation of berberine from Berberis lycium and its neuroprotective role in aluminium chloride induced rat model of Alzheimer's disease combined with insilico molecular docking.

Objective: Berberis lycium is an indigenous plant of Pakistan that is known for its medicinal properties. In the current study, we investigated the anti-Alzheimer's effect of berberine isolated from Berberis lycium.

Methods: Root extract of B.

Synthesis of amantadine clubbed -aryl amino thiazoles as potent urease, α-amylase & α-glucosidase inhibitors, kinetic and molecular docking studies.

A series of ten novel compounds were synthesized by incorporating a 1,3 thiazole core into amantadine and their structures were validated using different analytical and spectral methods such as FTIR, EI-MS, H NMR, and C NMR. The antibacterial and enzyme inhibitory properties of these newly synthesized compounds were evaluated. Remarkably, the compounds exhibited significant antibacterial activity against and .

Transforming Diagnosis and Therapeutics Using Cancer Genomics.

In past quarter of the century, much has been understood about the genetic variation and abnormal genes that activate cancer in humans. All the cancers somehow possess alterations in the DNA sequence of cancer cell's genome. In present, we are heading toward the era where it is possible to obtain complete genome of the cancer cells for their better diagnosis, categorization and to explore treatment options.

Synthesis, DNA binding and biological evaluation of benzimidazole Schiff base ligands and their metal(ii) complexes.

Two novel benzimidazole ligands ()-2-((4-(1-benzo[]imidazole-2-yl)phenylimino)methyl)-6-bromo-4-chlorophenol (L) and ()-1-((4-(1-benzo[]imidazole-2-yl)phenylimino)methyl)naphthalene-2-ol (L) with their corresponding Cu(ii), Ni(ii), Pd(ii) and Zn(ii) complexes were designed and synthesized. The compounds were characterized by elemental, IR, and NMR (H & C) spectral analyses. Molecular masses were determined by ESI-mass spectrometry, and the structure of ligand L was confirmed by single crystal X-ray diffraction analysis.

Investigation of Newly Synthesized Bis-Acyl-Thiourea Derivatives of 4-Nitrobenzene-1,2-Diamine for Their DNA Binding, Urease Inhibition, and Anti-Brain-Tumor Activities.

Bis-acyl-thiourea derivatives, namely -(((4-nitro-1,2-phenylene)bis(azanediyl)) bis(carbonothioyl))bis(2,4-dichlorobenzamide) (UP-1), -(((4-nitro-1,2-phenylene) bis(azanediyl))bis(carbonothioyl))diheptanamide (UP-2), and -(((4-nitro-1,2-phenylene)bis(azanediyl))bis(carbonothioyl))dibutannamide (UP-3), were synthesized in two steps. The structural characterization of the derivatives was carried out by FTIR, H-NMR, and C-NMR, and then their DNA binding, anti-urease, and anticancer activities were explored. Both theoretical and experimental results, as obtained by density functional theory, molecular docking, UV-visible spectroscopy, fluorescence (Flu-)spectroscopy, cyclic voltammetry (CV), and viscometry, pointed towards compounds' interactions with DNA.

Effects of against Streptozotocin-Aluminium Chloride Induced Alzheimer's Rats and Their In Silico Study.

is known for medicinal importance due to its antioxidant, antidiabetic, antidepressant, and anti-inflammatory properties. This study is aimed at evaluating the effect of seeds to cure Alzheimer's disease (AD). AD was induced in the rats with streptozotocin + aluminium chloride followed by treatment of methanolic extract of seeds.

Ethnomedicinal Plants with Protective Effects against Beta-Amyloid Peptide (Aβ)1-42 Indicate Therapeutic Potential in a New In Vivo Model of Alzheimer's Disease.

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder with unmet medical need. This investigation consisted of testing a range of ethanolic ethnomedicinal plant extracts (n = 18) traditionally used in the treatment of disorders such as anxiety, delirium, and memory loss. They were then screened for in vitro inhibitory activity against acetylcholinesterase (AChE), butylcholinesterase (BuChE), beta-secretase 1/beta-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1), and antioxidant activities.

Facile synthesis, crystal structure, biological evaluation, and molecular modeling studies of -((4-acetyl phenyl) carbamothioyl) pivalamide as the multitarget-directed ligand.

The crystal structure of -((4-acetylphenyl)carbamothioyl)pivalamide (3) was synthesized by inert refluxing pivaloyl isothiocyanate (2) and 4-aminoacetophenone in dry acetone. The spectroscopic characterization (H-NMR, CNMR, FT-IR) and single crystal assays determined the structure of synthesized compound (3). Systematic experimental and theoretical studies were conducted to determine the molecular characteristics of the synthesized crystal.

Evaluation of Phytochemistry and Pharmacological Properties of .

In the current study, the anti-inflammatory and analgesic potential of Alnus nitida (leaves and fruits) was evaluated in the Sprague-Dawley rat. Traditionally, A. nitida was used for the treatment of inflammatory ailments.

'Breast Cancer Resistance Likelihood and Personalized Treatment Through Integrated Multiomics'.

In recent times, enormous progress has been made in improving the diagnosis and therapeutic strategies for breast carcinoma, yet it remains the most prevalent cancer and second highest contributor to cancer-related deaths in women. Breast cancer (BC) affects one in eight females globally. In 2018 alone, 1.