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Zein 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 PDFAntiparasitic Activities of Acyl Hydrazones from Cinnamaldehydes and Structurally Related Fragrances.
Antibiotics (Basel)
November 2024
Organic Chemistry Laboratory, University Bayreuth, Universitätsstrasse 30, 95440 Bayreuth, Germany.
New drugs for the treatment of protozoal parasite infections such as toxoplasmosis and leishmaniasis are required. Cinnamaldehyde and its derivatives appear to be promising antiparasitic drug candidates. Acyl hydrazones of cinnamaldehyde, 4-dimethylaminocinnamaldehyde, and of the synthetic fragrances silvial and florhydral were prepared and tested for activity against () and () parasites.
View Article and Find Full Text PDFDeep Multitask Learning-Driven Discovery of New Compounds Targeting .
ACS Omega
December 2024
Laboratory of Cheminformatics, Faculty of Pharmacy, Universidade Federal de Goiás, Goiânia 74605-170, Brazil.
Article Synopsis
- Visceral leishmaniasis is a serious disease primarily found in low- and middle-income countries, with limited treatment options due to toxicity and drug resistance.
- Researchers developed a multitask learning (MTL) pipeline to predict the effectiveness of compounds against several species, screening about 1.3 million compounds and finding 20 potential candidates with significant antileishmanial activity.
- Three of these compounds showed strong efficacy and moderate safety, suggesting they could lead to new therapies, while the use of explainable models aids in understanding how these compounds work, potentially improving drug discovery for neglected tropical diseases.
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