A series of novel 6-thiopurine derivates containing 1,2,3-triazole were synthesized and their in vivo antimalarial activity and in vitro antileishmanial activity were examined. The compounds 10, 11, 12 and 14 presented higher values of inhibition of parasite multiplication than chloroquine. For antileishmanial activity, the compound 14 showed activity against the three species of Leishmania tested. None of compounds showed cytotoxicity against mammalian cells.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.biopha.2010.10.013 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Exploring the Potential of Malvidin and Echiodinin as Probable Antileishmanial Agents Through In Silico Analysis and In Vitro Efficacy.
Molecules
January 2025
Computational Biology and Chemistry Research Group, Vicerrectorado de Investigación, Universidad Católica de Santa María, Arequipa 04000, Peru.
Leishmaniasis, a neglected tropical disease caused by species, presents serious public health challenges due to limited treatment options, toxicity, high costs, and drug resistance. In this study, the in vitro potential of malvidin and echioidinin is examined as antileishmanial agents against , , and , comparing their effects to amphotericin B (AmpB), a standard drug. Malvidin demonstrated greater potency than echioidinin across all parasite stages and species.
View Article and Find Full Text PDFNew Insights into the Modifications and Bioactivities of Indole-3-Carboxaldehyde and its Derivatives as a Potential Scaffold for Drug Design: A Mini-Review.
Mini Rev Med Chem
January 2025
Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru 81310, Johor, Malaysia.
Indole, a ubiquitous structural motif in bioactive compounds, has played a pivotal role in drug discovery. Among indole derivatives, indole-3-carboxaldehyde (I3A) has emerged as a particularly promising scaffold for the development of therapeutic agents. This review delves into the recent advancements in the chemical modification of I3A and its derivatives, highlighting their potential applications in various therapeutic areas.
View Article and Find Full Text PDFZein Nanoparticles-Loaded Flavonoids-Rich Fraction from : Potential Antileishmanial Applications.
Pharmaceutics
December 2024
PostGraduate Program in Chemistry, Center for Exact Sciences and Technology (CCET), UFMA-Federal University of Maranhão, São Luís 65080-805, Brazil.
Leishmaniasis, caused by protozoa of the genus , is a major global health issue due to the limitations of current treatments, which include low efficacy, high costs, and severe side effects. This study aimed to develop a more effective and less toxic therapy by utilizing zein nanoparticles (ZNPs) in combination with a nonpolar fraction (DCMF) from (Syn. ), a plant rich in dimeric flavonoids called brachydins.
View Article and Find Full Text PDFInhibitory Effects of Sulfur Derivatives on Cell Viability and Secreted Acid Phosphatase In Vitro.
Microorganisms
December 2024
Department of Chemistry, Illinois State University, Normal, IL 61790, USA.
Sulfonamide drugs were the original class of antibiotics, demonstrating the antibacterial potential of dithiocarbazate and thiosemicarbazone Schiff base derivatives of syringaldehyde and 4-hydroxy-3,5-dimethylbenzaldehyde. We synthesized unique Schiff bases via the condensation of the aldehydes with hydrazine derivatives, which allows for the easy synthesis of several related compounds. These Schiff base derivatives were tested for antileishmanial properties against the parasitic protozoan .
View Article and Find Full Text PDFSynthesis and Structure-Activity Relationship of Thiourea Derivatives Against .
Pharmaceuticals (Basel)
November 2024
Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, Fundação Oswaldo Cruz, Rio de Janeiro 21040-900, Brazil.
Leishmaniasis, caused by protozoa and transmitted by vectors, presents varied clinical manifestations based on parasite species and host immunity. The lack of effective vaccines or treatments has prompted research into new therapies, including thiourea derivatives, which have demonstrated antiprotozoal activities. We synthesized two series of ,'-disubstituted thiourea derivatives through the reaction of isothiocyanates with amines.
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!