The present work reports the synthesis and biological activity of a series of 14 benzimidazole derivatives designed to act on the enzyme triosephosphate isomerase of Trypanosoma cruzi (TcTIM). This enzyme is involved in the metabolism of glucose, the only source of energy for the parasite. In this study, we found four compounds that inhibit TcTIM moderately and lack inhibitory activity against human TIM (HsTIM). In vitro studies against T. cruzi epimastigotes showed two compounds that were more active than the reference drug nifurtimox, and these presented a low cytotoxic effect in mouse macrophages (J744 cell line).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2015.08.018 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Elucidating the therapeutic potential of indazole derivative bindarit against K-ras receptor: An analysis using molecular dynamics exploration.
Biochem Biophys Rep
March 2025
School of Biosciences and Technology, Vellore Institute of Technology, Vellore, India.
Ras gene is frequently mutated in cancer. Among different subtypes of Ras gene, K-Ras mutation occurs in nearly 30 % of human cancers. K-Ras mutation, specifically K-Ras (G12D) mutation is prevalent in cancers like lung, colon and pancreatic cancer.
View Article and Find Full Text PDFFrustrated Lewis Pair Meets Polyhedral Oligomeric Silsesquioxane: Water-Tolerant Hybrid Porous Networks for Robust, Efficient, and Recyclable CO Catalysis.
ACS Appl Mater Interfaces
January 2025
State Key Laboratory of Molecular Engineering of Polymers, Fudan University, Shanghai 200433, China.
Frustrated Lewis pair chemistry (FLP) occupy a crucial position in nonmetal-mediated catalysis, especially toward activation of inert gas molecules. Yet, one formidable issue of homogeneous FLP catalysts is their instability on preservation and recycling. Here we contribute a general solution that marries the polyhedral oligomeric silsesquioxane (POSS) with a structurally specific frustrated Lewis acid to fabricate porous polymer networks, which can form water-insensitive heterogeneous FLP catalysts upon employing Lewis base substrates.
View Article and Find Full Text PDFEgg reappearance periods associated with anthelmintic treatments given to horses in winter and summer over two years.
Vet Parasitol Reg Stud Reports
January 2025
Tāwharau Ora - School of Veterinary Science, Massey University, Private Bag 11222, Palmerston North 4410, New Zealand.
Shortened egg reappearance periods (ERP) have been seen as an early warning of anthelmintic resistance development in cyathostomins in horses. The hypothesis has been that in these instances, efficacy against egg laying adult cyathostomins remains high, but a decline in activity against later larval stages leads to the earlier resumption of egg shedding after treatment. In this study using a single herd of horses we investigated the ERP of a number of commonly used equine anthelmintics and examined whether ERP might show seasonal variation between winter and summer.
View Article and Find Full Text PDFIn silico and in vitro assessments of the mutagenicity of the azilsartan photoproduct.
Mutat Res Genet Toxicol Environ Mutagen
January 2025
Research & Development, Kongo Chemical Co., Ltd, Himata, Toyama 9300912, Japan.
Photodegradation of azilsartan yields a phenanthridine derivative (APP). We suspected that APP could be a DNA-reactive substance, since many phenanthridine derivatives are mutagenic. In silico quantitative structure-activity relationship analysis indicated potential mutagenicity of APP, due to DNA reactivity at the 6-aminophenanthridine moiety.
View Article and Find Full Text PDFTargeting tubulin protein to combat fungal disease: Design, synthesis, and its new mechanistic insights of benzimidazole hydrazone derivatives.
Int J Biol Macromol
January 2025
State Key Laboratory of Green Pesticides, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China. Electronic address:
As the vital the biomacromolecule in eukaryotic cells, tubulin protein is essential for preserving cell shape, facilitating cell division, and cell viability. Tubulin has been approved as promising target for anticancer, and antifungal therapy. However, there are still many gaps in tubulin-targeted fungicidal discovery.
View Article and Find Full Text PDFWant 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!