Results 21 to 30 of about 3,959 (186)

Repositioning FDA-Approved Sulfonamide-Based Drugs as Potential Carbonic Anhydrase Inhibitors in Trypanosoma cruzi: Virtual Screening and In Vitro Studies [PDF]

Pharmaceuticals
Background/Objectives: α-carbonic anhydrase (α-TcCA) has emerged as a promising drug target in T. cruzi, the causative agent of Chagas disease in the Americas. Sulfonamides, known inhibitors of CAs, bind to the zinc ion on the enzyme’s active site.
Eyra Ortiz-Pérez, Adriana Moreno-Rodríguez, Timoteo Delgado-Maldonado, Jessica L. Ortega-Balleza, Alonzo González-González, Alma D. Paz-González, Karina Vázquez, Guadalupe Avalos-Navarro, Simone Giovannuzzi, Claudiu T. Supuran, Gildardo Rivera   +10 more
doaj   +2 more sources

Evaluation of proline analogs as trypanocidal agents through the inhibition of a Trypanosoma cruzi proline transporter [PDF]

Biochimica Et Biophysica Acta - General Subjects, 2017
Background: Trypanosoma cruzi, the etiological agent of Chagas disease, uses proline as its main carbon source, essential for parasite growth and stage differentiation in epimastigotes and amastigotes.
Melisa Saye, Lucia Fargnoli, Chantal Reigada   +2 more
exaly   +2 more sources

A trypanosome oligopeptidase as a target for the trypanocidal agents pentamidine, diminazene and suramin [PDF]

FEBS Letters, 1998
African trypanosomes contain a cytosolic serine oligopeptidase, called OP-Tb, that is reversibly inhibited by the active principles of three of the five most commonly used trypanocidal drugs: pentamidine, diminazene and suramin.
Troeberg, Linda, Nickel, Peter, Jones, Roy, Rory E. Morty, Linda Troeberg, Theresa H.T. Coetzer, Lonsdale-Eccles, John D., John D. Lonsdale-Eccles, Roy Jones, Pike, Robert N., Morty, Rory E., Robert N. Pike, Peter Nickel, Coetzer, Theresa H.T.   +13 more
core   +3 more sources

Schistosomicidal and trypanocidal structure–activity relationships for (±)-licarin A and its (−)- and (+)-enantiomers

Phytochemistry, 2011
(+/-)-Licarin A (1) was obtained by oxidative coupling, and its enantiomers, (-)-licarin A (2) and (+)-licarin A (3), were resolved by chiral HPLC.
Lizandra G MAGALHÃES, Priscilla P Luz, Ademar A Da Silva Filho   +2 more
exaly   +2 more sources

Chemical and biological analysis of 4-acyloxy-3-nitrocoumarins as trypanocidal agents [PDF]

Arabian Journal of Chemistry, 2021
Chagas disease is the most widespread contagious tropical disease in Latin America, being an important public health problem. Treatments against this disease are still very ineffective, presenting several side effects.
Salgado, Francisco, Liempi, Ana, Matos, María J., Matos, Maria João Correia Pinto Carvalho de, Pozo Martínez, Josué Santiago, Borges, Fernanda, Olea Azar, Claudio, Maya Arango, Juan Diego, Jaque Olmedo, Pablo César, Olea Azar, Claudio Alberto, Uriarte Villares, Eugenio, Pozo Martínez, Josué, Moncada Basualto, Mauricio Javier, Moncada Basualto, Mauricio, Uriarte, Eugenio, Maya, Juan Diego, Salgado, Francisco J., Jaque, Pablo, Kemmerling Weis, Ulrike, Kemmerling, Ulrike   +19 more
core   +4 more sources

Evaluation of substituted ebselen derivatives as potential trypanocidal agents. [PDF]

Bioorg Med Chem Lett, 2017
Human African trypanosomiasis is a disease of sub-Saharan Africa, where millions are at risk for the illness. The disease, commonly referred to as African sleeping sickness, is caused by an infection by the eukaryotic pathogen, Trypanosoma brucei. Previously, a target-based high throughput screen revealed ebselen (EbSe), and its sulfur analog, EbS, to ...
Gordhan HM, Patrick SL, Swasy MI, Hackler AL, Anayee M, Golden JE, Morris JC, Whitehead DC.   +7 more
europepmc   +4 more sources

Exploring 6-Hydroxy-3-Aryl/Heteroarylcoumarins as Promising Candidates Against Trypanosoma cruzi. [PDF]

ChemMedChem
New therapies are urgently needed for Chagas disease, and screening of 6‐hydroxy‐3‐aryl/heteroarylcoumarin derivatives identified highly selective compounds with potent activity against T. cruzi. In particular, derivative 1f showed submicromolar trypomastigote potency, dual‐stage activity, and inhibition of amastigote‐to‐trypomastigote differentiation,
Pereira CN, Lara LDS, Lanera SDC, Souza TP, Pereira MCS, Delogu GL, Santos MSD, Matos MJ.   +7 more
europepmc   +2 more sources

Trypanocidal Effects of Polyprenylated Benzophenone Enriched Brazilian Red Propolis Extract and Its Isolated Constituent. [PDF]

Chem Biodivers
In vitro trypanocidal activity of a polyprenylated benzophenone‐enriched Brazilian red propolis extract (SEBz) and its major constituents, guttiferone E/xanthochymol (GUT/XAN) and oblongifolin B (OBL), exhibit in vitro trypanocidal activity against Trypanosoma cruzi, inducing ultrastructural damage with moderate cytotoxicity and no significant ...
Oliveira ND, Pagotti MC, Paula LAL, Paixão MZ, Albino Dos Santos D, de Freitas RF, Ambrósio SR, Veneziani RCS, Bastos JK, Magalhães LG.   +9 more
europepmc   +2 more sources

Synthesis of 4-(4-chlorophenyl)thiazole compounds: in silico and in vitro evaluations as leishmanicidal and trypanocidal agents [PDF]

Anais da Academia Brasileira de Ciências, 2023
Neglected tropical diseases are a diverse group of communicable pathologies that mainly prevail in tropical and subtropical regions. Thus, the objective of this work was to evaluate the biological potential of eight 4-(4-chlorophenyl)thiazole compounds ...
IRANILDO JOSÉ DA CRUZ FILHO, JAMERSON F. DE OLIVEIRA, ALINE CAROLINE S. SANTOS, VALÉRIA R.A. PEREIRA, MARIA CARMO A. DE LIMA   +4 more
doaj   +1 more source

In Vitro Antitrypanosomal and Antibacterial Activity of Aqueous, Hydroethanolic and Ethanolic Extracts of Rumex obtusifolius L. Leaf and Root. [PDF]

Basic Clin Pharmacol Toxicol
ABSTRACT Plant extracts are an important raw material for the development of new drugs. Rumex obtusifolius L., popularly known as ‘bitter dock’, has significant pharmacological properties. This study evaluated the in vitro antitrypanosomal activity of aqueous, hydroethanolic and ethanolic extracts from the leaf and roots of R. obtusifolius L.
Borges GK, Das Neves GB, Reichardt L, Costa UMD, Miletti LC, Bastos-Pereira AL.   +5 more
europepmc   +2 more sources