Imidazo[2,1-b]thiazole carbohydrate derivatives: Synthesis and antiviral activity against Junin virus, agent of Argentine hemorrhagic fever.

Eur J Med Chem

CIHIDECAR-CONICET - Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Pabellón II - Ciudad Universitaria, 1428 Buenos Aires, Argentina.

Published: January 2011

Herein, we describe the syntheses of 3,5-disubstituted imidazo[2,1-b]thiazole. The cyclization step was performed in two different conditions by using either thermal or microwave heating. Comparing the results of both methodologies, we found that the microwave assistance is an improved alternative to obtain this family of heterocyclic compound. Compounds were first evaluated for cytotoxicity in Vero cells by MTT method and then, the antiviral activity was assayed by a virus yield inhibition assay in the range of concentrations lower than the corresponding CC(50), using JUNV strain IV4454 as the model system. The most active compounds (3 and 4), showed a level of antiviral activity against JUNV in monkey Vero cells better than the reference substance ribavirin. Then, they are promising lead compound for further analysis and characterization to establish their therapeutic potential against hemorrhagic fever viruses.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejmech.2010.11.012DOI Listing

Publication Analysis

Top Keywords

antiviral activity
12
hemorrhagic fever
8
vero cells
8
imidazo[21-b]thiazole carbohydrate
4
carbohydrate derivatives
4
derivatives synthesis
4
synthesis antiviral
4
activity junin
4
junin virus
4
virus agent
4

Similar Publications

Bacteriocins, a class of molecules produced by bacteria, exhibit potent antimicrobial properties, including antiviral activities. The urgent need for treatments against SARS-CoV-2 has proposed bacteriocins such as enterocin DD14 (EntDD14) as potential therapeutic agents. However, the mechanism of macromolecular interaction of EntDD14 for the inhibition of SARS-CoV-2 is not yet fully understood, and its efficacy against variants like JN.

View Article and Find Full Text PDF

Modular cascade with engineered HpaB for efficient synthesis of hydroxytyrosol.

Bioorg Chem

January 2025

College of Biological Science and Engineering, Fuzhou University, Fuzhou 350108 China; Institute of Enzyme Catalysis and Synthetic Biotechnology, Fuzhou University, Fuzhou 350108 China. Electronic address:

Hydroxytyrosol, a naturally occurring chemical with antioxidant and antiviral properties, is widely used in the nutrition, pharmaceutical, and cosmetic industries. In the present study, a modularized cascade composed of Modules 1 and 2 was designed and implemented to convert l-tyrosine to hydroxytyrosol. Module 1 was a four-enzymatic cascade for converting l-tyrosine to tyrosol.

View Article and Find Full Text PDF

Structure-based discovery of dual-target inhibitors of the helicase from bagaza virus.

Int J Biol Macromol

January 2025

Department of Cardiology, the First hospital of Shanxi Medical University, and MOE Key Laboratory of Cellular Physiology at Shanxi Medical University, Taiyuan, China. Electronic address:

Bagaza virus (BAGV) is a mosquito-borne flavivirus and has caused significant avian death in many regions, and also garnered recognition as a significant human pathogen causing diseases like encephalitis. The genome of BAGV encodes ten proteins including three structural proteins and seven nonstructural proteins. The C-terminus of the BAGV NS3 helicase serves as a helicase during BAGV replication, aiding in ATP hydrolysis and unwinding of double-stranded RNA.

View Article and Find Full Text PDF

Exploring the mechanism and crosstalk between IL-6 and IL- 1β on M2 macrophages under metabolic stress conditions.

Cytokine

January 2025

Department of Basic Sciences, Institute of Fisheries Post Graduate Studies, Tamil Nadu Dr. J. Jayalalithaa Fisheries University (TNJFU), OMR Campus, Vaniyanchavadi, Chennai 603103, Tamil Nadu, India. Electronic address:

Macrophages are highly variable immune cells that are important in controlling inflammation and maintaining tissue balance. The ability to polarize into two major types-M1, promoting inflammation, and M2, resolving inflammation and contributing to tissue repair-determines their specific roles in health and disease. M2 macrophages are particularly important for reducing inflammation and promoting tissue regeneration, but their function is shaped mainly by surrounding cells.

View Article and Find Full Text PDF

Nitroxoline evidence amoebicidal activity against Acanthamoeba castellanii through DNA damage and the stress response pathways.

Int J Parasitol Drugs Drug Resist

January 2025

Department of Medical Microbiology and Parasitology, School of Basic Medical Sciences, Fudan University, Shanghai, China. Electronic address:

Acanthamoeba castellanii is a widespread unicellular eukaryote found in diverse environments, including tap water, soil, and swimming pools. It is responsible for severe infections, such as Acanthamoeba keratitis and granulomatous amebic encephalitis, particularly in individuals with immunocompromisation. The ability of protozoans to form dormant and persistent cysts complicates treatment, as current therapies are ineffective against cyst stages and suffer from poor specificity and side effects.

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!