A5059486375- Adenosine and Purinergic Signaling
- Synthesis and Biological Evaluation
- Bioactive Compounds and Antitumor Agents
- Computational Drug Discovery Methods
- Click Chemistry and Applications
- Adolescent and Pediatric Healthcare
- Eosinophilic Esophagitis
- Pregnancy and Medication Impact
- Carbohydrate Chemistry and Synthesis
- Mast cells and histamine
- Moringa oleifera research and applications
- Parasites and Host Interactions
- Neurological Complications and Syndromes
- CRISPR and Genetic Engineering
- Fluorine in Organic Chemistry
- Insect Pest Control Strategies
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Marine Sponges and Natural Products
- Chemical synthesis and alkaloids
- Biomedical and Engineering Education
- Trypanosoma species research and implications
- Animal Nutrition and Physiology
- RNA and protein synthesis mechanisms
- Science, Research, and Medicine
- Proteins in Food Systems
Universidade Federal do Rio de Janeiro
2017-2025
Fundação Oswaldo Cruz
2024
Universidade Federal Fluminense
2017-2022
Background/objectives: Schistosomiasis is caused by flatworms of the genus Schistosoma, for which mollusks Biomphalaria are intermediate hosts. Niclosamide (NCL) a molluscicide recommended World Health Organization (WHO) control Biomphalaria. Although effective, it expensive and environmentally toxic, raises concerns regarding its widespread use. As result, we explored new synthetic substances as alternative strategies controlling glabrata. We evaluated molluscicidal activity...
P2X7R is a purinergic receptor with broad expression throughout the body, especially in immune system cells. activation causes inflammatory mediators to release, including interleukin-1β (IL-1β), processing and release of which are critically dependent on this ion channel activation. P2X7R's therapeutic potential augments discovery new antagonistic compounds. Thus, we investigated whether Eugenia sulcata essential oil could block activity. The (ESO) dose-dependently inhibited ATP-promoted PI...
Twenty new 2-(1H-pyrazol-1-yl)-1,3,4-thiadiazole analogs were synthetized to develop P2X7 receptor (P2X7R) inhibitors. P2X7R inhibition in vitro was evaluated mouse peritoneal macrophages, HEK-293 cells transfected with hP2X7R (dye uptake assay), and THP-1 (IL-1β release assay). The 1-(5-phenyl-1,3,4-thiadiazol-2-yl)-1H-pyrazol-5-amine derivatives 9b, 9c, 9f, 2-(3,5-dimethyl-1H-pyrazol-1-yl)-5-(4-fluorophenyl)-1,3,4-thiadiazole (11c) showed inhibitory effects IC50 values ranging from 16 122...
HIV-1 infection is a global epidemic whose treatment limited majorly by viral resistance and adverse effects. Natural products from algae have been studied for many years, including antiviral, being an alternative to anti-HIV drug design. Since the isolation of natural can be hurdle, molecular modeling important tool study these compounds. Herein, structure-activity relationship, docking, dynamic studies were performed direct ten marine with activity. In descriptors identified associating...
Schistosomiasis is caused by the intestinal parasite Schistosoma mansoni . Individuals are affected schistosomiasis when they exposed to aquatic environments contaminated with cercariae that emerged from infected intermediate host mollusk of genus Biomphalaria The WHO recommends using molluscicidal products reduce snail population and disease transmission. encourages search for alternative substances in control. Natural seen as a promising because abundant countries where endemic have many...
ATP acts in the extracellular environment as an important signal, activating a family of receptors called purinergic receptors. In recent years, interest potential therapeutics components, including agonists and antagonists receptors, has increased. Currently, many observations have indicated that mediator inflammatory responses and, when found high concentrations space, is related to activation P2X7 receptor. this sense, search for new inhibitors receptor attracted great deal attention...
Purinergic receptors are transmembrane proteins responsive to extracellular nucleotides and expressed by several cell types throughout the human body. Among all identified subtypes, P2×7 receptor has emerged as a relevant target for treatment of inflammatory disease. Several clinical trials have been conducted evaluate effectiveness P2×7R antagonists. However, date, no selective antagonist reached use. In this work, we report pharmacological evaluation eleven N, S-acetal juglone derivatives...
Abstract The pathogenic complexity of Alzheimer's disease (AD) demands the development multitarget‐directed agents aiming at improving actual pharmacotherapy. Based on cholinergic hypothesis and considering well‐established role butyrylcholinesterase (BuChE) in advanced stages AD, chemical structure acetylcholinesterase (AChE) inhibitor drug donepezil ( 1 ) was rationally modified for design new N ‐benzyl‐piperidine derivatives 4a−d as potential multitarget‐direct AChE BuChE inhibitors....
Infections by Candida albicans in immune compromised patients cause significant morbidity and mortality. In the search for potential molecular targets drug development, family of agglutinin-like proteins (Als) C. have been identified due to numerous attributes associated with high virulence, most prominently their role adherence. Here, models individual members Als illustrated common unique structure features. Additionally, dynamic simulations were performed display regions mobility. The...
Schistosomiasis is a tropical disease transmitted in an aqueous environment by cercariae from the Schistosoma genus. This affects 200 million people living risk areas around world. The control of schistosomiasis realized chemotherapy, wastewater sanitation, health education, and mollusk using molluscicidal agents. work evaluates effects nanoemulsion containing essential oil Myrciaria floribunda leaves as cercaricidal agent against Biomphalaria glabrata mollusks mansoni cercariae. showed...
Microbial resistance has become a worldwide public health problem and may lead to morbidity mortality in affected patients.Therefore, this work aimed evaluate the antibacterial activity of quinone-4- oxoquinoline derivatives.These derivatives were evaluated against Gram-positive Gram-negative bacteria by their activity, anti-biofilm, hemolytic activities silico assays.The quinone-4-oxoquinoline presented broad-spectrum and, some cases, more active than commercially available reference drugs....