AI Article Synopsis

Article Abstract

Chagas disease and leishmaniasis are vector-borne infectious diseases affecting both humans and animals. These neglected tropical diseases can be fatal if not treated. Hundreds to thousands of new Chagas disease and leishmaniasis cases are being reported by the WHO every year, and currently available treatments are insufficient. Severe adverse effects, impractical administrations and increased pathogen resistance against current clinical treatments underscore a serious need for the development of new drugs to curb these ailments. In search for such drugs, we investigated a series of nitrofuran-based azine derivatives. Herein, we report the design, synthesis, electrochemistry, and biological activity of these derivatives against promastigotes and amastigotes of , and strains, as well as epimastigotes and trypomastigotes of . Two leishmanicidal early leads and one trypanosomacidal hit with submicromolar activity were uncovered and stand for further investigation in the search for new antitrypanosomatid drugs. Future objective will focus on the identification of involved biological targets with the parasites.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10583827PMC
http://dx.doi.org/10.1039/d3md00220aDOI Listing

Publication Analysis

Top Keywords

design synthesis
8
synthesis electrochemistry
8
chagas disease
8
disease leishmaniasis
8
electrochemistry anti-trypanosomatid
4
anti-trypanosomatid hit/lead
4
hit/lead identification
4
identification nitrofuranylazines
4
nitrofuranylazines chagas
4
leishmaniasis vector-borne
4

Similar Publications

Adherence to Oral Anticancer Agents Among Adults With Gastrointestinal Tract Cancer: A Scoping Review.

Cancer Nurs

January 2025

Author Affiliations: The Nethersole School of Nursing, Faculty of Medicine, Chinese University of Hong Kong, Shatin, Hong Kong (Ms Chen and Drs Ng, Zhang, and Chan); and Nursing Department, People's Hospital of Guangxi Zhuang Autonomous Region, Guangxi Academy of Medical Sciences, Nanning, China (Ms Chen).

Background: Patients with gastrointestinal tract cancer reported suboptimal adherence to oral anticancer agents (OAAs), reducing their therapeutic benefit and increasing mortality risk. A scoping review can comprehensively map available evidence on adherence to OAAs and inform appropriate support to improve treatment outcomes.

Objective: The aim of this study was to comprehensively map studies on adherence to OAAs among adults with gastrointestinal tract cancer, including the adherence rate, nonadherence reasons, influential factors, management strategies, and theories that guide these studies.

View Article and Find Full Text PDF

Small and Versatile Cyclotides as Anti-infective Agents.

ACS Infect Dis

January 2025

Programa de Pós-Graduação em Biotecnologia, Universidade Católica Dom Bosco, Campo Grande, Mato Grosso do Sul 79117-900, Brazil.

Plants provide an abundant source of potential therapeutic agents, including a diverse array of compounds, such as cyclotides, which are peptides known for their antimicrobial activity. Cyclotides are multifaceted molecules with a wide range of biological activities. Their unique topology forms a head-to-tail cyclic structure reinforced by a cysteine knot, which confers chemical and thermal stability.

View Article and Find Full Text PDF

Background: Early childhood is a critical period for shaping lifelong health behaviors, making early childhood education and care (ECEC) environments ideal for implementing nutrition and physical activity interventions. eHealth tools are increasingly utilized in ECEC settings due to their accessibility, scalability, and cost-effectiveness, demonstrating promise in enhancing educators' practices. Despite the potential effectiveness of these eHealth approaches, a comprehensive collection of available evidence on eHealth tools designed to assess or support best practices for nutrition or physical activity in ECECs is currently lacking.

View Article and Find Full Text PDF

Objective: To provide an updated synthesis on effects of glucagon-like peptide 1 receptor agonists (GLP-1 RAs) on weight, BMI, and waist circumference incorporating newer randomized controlled trials (RCTs), particularly in individuals with overweight or obesity.

Research Design And Methods: We systematically searched PubMed, Embase, and Cochrane Central Register of Controlled Trials (CENTRAL) for RCTs published from inception to 4 October 2024. The search was limited to RCTs evaluating the use of GLP-1 RAs for mean differences from baseline in weight, BMI, and waist circumference in adults with obesity or overweight with or without diabetes.

View Article and Find Full Text PDF

Designing binders to target undruggable proteins presents a formidable challenge in drug discovery. In this work, we provide an algorithmic framework to design short, target-binding linear peptides, requiring only the amino acid sequence of the target protein. To do this, we propose a process to generate naturalistic peptide candidates through Gaussian perturbation of the peptidic latent space of the ESM-2 protein language model and subsequently screen these novel sequences for target-selective interaction activity via a contrastive language-image pretraining (CLIP)-based contrastive learning architecture.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!