The synthesis of vinylogous of 1,2-dithiole-3-thione is described. The activity in experimental schistosomiasis (schistosomicidal activity) was tested with mice infected with Schistosoma mansoni. The reference compound was 4-methyl-5-(pyrazinyl)-1,2-dithiole-3-thione (oltipraz).
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Molecules
January 2025
Centro de Ciências Naturais e Humanas, Universidade Federal do ABC, Santo André 09280-560, SP, Brazil.
In the present study, the hexane extract from branches of (Winteraceae) displayed potent activity against parasites (100% mortality of the worms at 200 μg/mL). Bioactivity-guided fractionation afforded, in addition to the previously reported bioactive sesquiterpene 3,6-epidioxy-bisabola-1,10-diene, two chemically related drimane sesquiterpenes-polygodial () and 9-deoxymuzigadial (). The anti- effects for compounds and were determined in vitro, with compound demonstrating significant potency (EC value of 10 μM for both male and female worms), while was inactive.
View Article and Find Full Text PDFFront Parasitol
April 2024
Institut für Parasitologie, Biomedizinisches Forschungszentrum Seltersberg (BFS), Justus Liebig Universitaet Giessen, Giessen, Germany.
Introduction: Schistosomiasis has for many years relied on a single drug, praziquantel (PZQ) for treatment of the disease. Immense efforts have been invested in the discovery of protein kinase (PK) inhibitors; however, given that the majority of PKs are still not targeted by an inhibitor with a useful level of selectivity, there is a compelling need to expand the chemical space available for synthesizing new, potent, and selective PK inhibitors. Small-molecule inhibitors targeting the ATP pocket of the catalytic domain of PKs have the potential to become drugs devoid of (major) side effects, particularly if they bind selectively.
View Article and Find Full Text PDFExp Parasitol
January 2025
Faculty of Pharmacy, Department of Pharmaceutical Sciences, Federal University of Juiz de Fora, Juiz de Fora, MG, 36036-900, Brazil. Electronic address:
Schistosomiasis stands as one of the most significant parasitic diseases on a global scale, with approximately 250 million infections worldwide. It is imperative to address this pressing issue by developing new antischistosomal drugs. Chalcones have emerged as a promising class of natural compounds, demonstrating noteworthy effects observed in vitro experiments with Schistosoma mansoni, and demonstrating the ability to inhibit SmNTPDases and apyrase from potatoes.
View Article and Find Full Text PDFBiomedicines
December 2024
Infectious and Tropical Diseases Research Group (e-INTRO), Biomedical Research Institute of Salamanca, Research Centre for Tropical Diseases at the University of Salamanca (IBSAL-CIETUS), Faculty of Pharmacy, University of Salamanca, 37007 Salamanca, Spain.
Background: Schistosomiasis impacts over 230 million people globally, with 251.4 million needing treatment. The disease causes intestinal and urinary symptoms, such as hepatic fibrosis, hepatomegaly, splenomegaly, and bladder calcifications.
View Article and Find Full Text PDFPhytomedicine
January 2025
Jinan Central Hospital, Shandong First Medical University, Jinan 250013, Shandong, China. Electronic address:
Background: The dysregulation of ribosome biogenesis has been extensively identified in various cancers, making it emerge as a hallmark of malignant cells. This highlights the potential of targeting ribosome biogenesis as an effective approach for treating cancer patients. Although chemotherapy drugs including doxorubicin and cisplatin often target ribosome biogenesis to induce DNA damage or inhibit tumor cell proliferation, they are associated with significant side effects.
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