Current chemotherapy drugs for Chagas' disease are insufficient due to their limited efficacy; however, anti-trypanosomal agents have recently shown promise. As such, synthetic intermediates of komaroviquinone were evaluated for anti-trypanosomal activity. Based on the results, a series of novel quinone derivatives were screened for anti-trypanosomal activity and mammalian cytotoxicity. Several quinone derivatives displayed higher antiprotozoal activity against Trypanosoma cruzi trypomastigotes than the reference drug benznidazole, without concomitant toxicity toward the host cell.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2015.05.022 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Discovery of Trypanosoma brucei inhibitors enabled by a unified synthesis of diverse sulfonyl fluorides.
Commun Chem
October 2024
School of Chemistry and Astbury Centre for Structural Molecular Biology, University of Leeds, Leeds, LS2 9JT, UK.
Sets of electrophilic probes are generally prepared using a narrow toolkit of robust reactions, which tends to limit both their structural and functional diversity. A unified synthesis of skeletally-diverse sulfonyl fluorides was developed that relied upon photoredox-catalysed dehydrogenative couplings between hetaryl sulfonyl fluorides and hydrogen donor building blocks. A set of 32 diverse probes was prepared, and then screened against Trypanosoma brucei.
View Article and Find Full Text PDFActivity of pyridyl-pyrazolone derivatives against Trypanosoma cruzi.
Exp Parasitol
July 2024
Laboratório de Biologia Celular, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz (FIOCRUZ), Rio de Janeiro, 210360-040, Brazil. Electronic address:
New affordable drugs are needed for the treatment of infection with the protozoan parasite Trypanosoma cruzi responsible for the Chagas disease (CD). Only two old drugs are currently available, nifurtimox and benznidazole (Bz) but they exhibit unwanted side effects and display a weak activity in the late chronic phase of the disease. In this context, we evaluated the activity of a series of aryl-pyrazolone derivatives against T cruzi, using both bloodstream trypomastigote and intracellular amastigote forms of the parasite.
View Article and Find Full Text PDFSaturated Iso-Type Fatty Acids from the Marine Bacterium with Anti-Trypanosomal Potential.
Pharmaceuticals (Basel)
April 2024
Pathophysiology Laboratory, Instituto Butantan, Av. Vital Brazil, 1500, Sao Paulo 05503-900, SP, Brazil.
Chagas disease is a Neglected Tropical Disease with limited and ineffective therapy. In a search for new anti-trypanosomal compounds, we investigated the potential of the metabolites from the bacteria living in the corals and sediments of the southeastern Brazilian coast. Three corals, , , and sediments yielded 11 bacterial strains that were fully identified by MALDI-ToF/MS or gene sequencing, resulting in six genera-, , , , and To conduct this study, EtOAc extracts were prepared and tested against The crude extracts showed IC values ranging from 15 to 51 μg/mL against the trypomastigotes.
View Article and Find Full Text PDFAnti-trypanosomal Lignans Isolated from Salvadoran .
J Nat Prod
April 2024
Faculty of Pharmacy, Keio University, 1-5-30, Shibakoen, Minato-ku, Tokyo 105-8512, Japan.
A search for anti-trypanosomal natural compounds from plants collected in El Salvador, a country particularly endemic for Chagas disease, resulted in the isolation of five lignan-type compounds (-) from . The lignan derivatives , , and are new. Their absolute configuration was determined by chemical derivatization.
View Article and Find Full Text PDFChemoselective Synthesis and Anti-Kinetoplastidal Properties of 2,6-Diaryl-4-tetrahydro-thiopyran-4-one -Oxides: Their Interplay in a Cascade of Redox Reactions from Diarylideneacetones.
Molecules
April 2024
UMR7042 Université de Strasbourg-CNRS-UHA, Laboratoire d'Innovation Moléculaire et Applications (LIMA), Team Bio(IN)organic and Medicinal Chemistry, European School of Chemistry, Polymers and Materials (ECPM), 25 Rue Becquerel, F-67087 Strasbourg, France.
2,6-Diaryl-4-tetrahydro-thiopyran-4-ones and corresponding sulfoxide and sulfone derivatives were designed to lower the major toxicity of their parent anti-kinetoplatidal diarylideneacetones through a prodrug effect. Novel diastereoselective methodologies were developed and generalized from diarylideneacetones and 2,6-diaryl-4-tetrahydro-thiopyran-4-ones to allow the introduction of a wide substitution profile and to prepare the related -oxides. The in vitro biological activity and selectivity of diarylideneacetones, 2,6-diaryl-4-tetrahydro-thiopyran-4-ones, and their -sulfoxide and sulfone metabolites were evaluated against , , and various species in comparison with their cytotoxicity against human fibroblasts MRC-5.
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!