Probing Adamantane Arylhydroxamic Acids against Trypanosoma brucei and Trypanosoma cruzi
In this work, we present the synthesis and the anti-trypanosomal activity of the 2-(4-(adamant-1-yl)phenyl)-N-hydroxyarylamides, 1a,b and the 2-(4-(adamant-1-yl)phenoxy)-N-hydroxyacetamide, 1c.
Angeliki Sofia Foscolos +4 more
doaj +1 more source
Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities [PDF]
The synthesis, cytotoxicity, anti-leishmanial and anti-trypanosomal activities of twelve triclosan-caffeic acid hybrids are described herein. The structure of the synthesized products was elucidated by a com- bination of spectrometric analyses.
Agut, Raúl +8 more
core +1 more source
Hinokinin, an Emerging Bioactive Lignan
Hinokinin is a lignan isolated from several plant species that has been recently investigated in order to establish its biological activities. So far, its cytotoxicity, its anti-inflammatory and antimicrobial activities have been studied.
Maria Carla Marcotullio +2 more
doaj +1 more source
Metabolomics-guided isolation of anti-trypanosomal metabolites from the endophytic fungus Lasiodiplodia theobromae [PDF]
Fungal endophytes offer diverse and unique secondary metabolites, making these organisms potential sources of promising drug leads. The application of high-resolution-liquid chromatography mass spectrometry and nuclear magnetic resonance-based ...
Clements, Carol J. +3 more
core +1 more source
Beta-carboline is an indole alkaloid which has been identified as a valuable heterocyclic nucleus in the field of medicinal chemistry. It has different biological activities like antibacterial, anticancer, antifungal, antimalarial, antileishmanial, anti ...
Mahender Thatikayala +6 more
doaj +1 more source
Nifurtimox Is Effective Against Neural Tumor Cells and Is Synergistic with Buthionine Sulfoximine. [PDF]
Children with aggressive neural tumors have poor survival rates and novel therapies are needed. Previous studies have identified nifurtimox and buthionine sulfoximine (BSO) as effective agents in children with neuroblastoma and medulloblastoma.
Du, Michael +4 more
core +1 more source
Evaluation of the Trypanosoma brucei 6-oxopurine salvage pathway as a potential target for drug discovery. [PDF]
Due to toxicity and compliance issues and the emergence of resistance to current medications new drugs for the treatment of Human African Trypanosomiasis are needed. A potential approach to developing novel anti-trypanosomal drugs is by inhibition of the
Eva Doleželová +9 more
doaj +1 more source
Bisguanidine, Bis(2-aminoimidazoline), and Polyamine Derivatives as Potent and Selective Chemotherapeutic Agents against Trypanosoma brucei rhodesiense. Synthesis and in Vitro Evaluation [PDF]
The in vitro screening for trypanocidal activity against Trypanosoma brucei rhodesiense of an in-house library of 62 compounds [i.e. alkane, diphenyl, and azaalkane bisguanidines and bis-(2-aminoimidazolines)], which were chosen for their structural ...
Brun, Reto, Dardonville, Christophe
core +2 more sources
Nitroheterocyclic drug resistance mechanisms in Trypanosoma brucei [PDF]
OBJECTIVES: The objective of this study was to identify the mechanisms of resistance to nifurtimox and fexinidazole in African trypanosomes. METHODS: Bloodstream-form Trypanosoma brucei were selected for resistance to nifurtimox and fexinidazole by ...
Berriman, Matthew +5 more
core +3 more sources
Peptidomimetic Vinyl Heterocycle Inhibitors of Cruzain Effect Anti-Trypanosomal Activity.
Cruzain, an essential cysteine protease of the parasitic protozoan, Trypanosoma cruzi, is an important drug target for Chagas disease. We describe here a new series of reversible, but time-dependent, inhibitors of cruzain, composed of a dipeptide ...
B. Chenna +12 more
semanticscholar +1 more source

