Results 21 to 30 of about 7,518 (197)

Terpenoid Derivatives as Potential Trypanocidal Agents [PDF]

Medicinal chemistry, 2016
In this review we refer to a promising family of molecules in the fight against Chagas disease. Terpene derivatives are abundant in the plant Kingdom and in the last years many compounds have shown important biological activities. Diterpenes and sesquiterpene lactones have shown in vitro and in vivo trypanocidal activity and they emerge as potential ...
Lozano E, Barrera P
openaire   +3 more sources

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

Scalable Access to N‑Acylindole Linkages: Enabling the Synthesis of Antitrypanosomal Noncanonical Cyclic Peptides for Chagas Disease. [PDF]

Angew Chem Int Ed Engl
A gram‐scale supply of bulbiferamide A, which features a rare N‐acylindole linkage and possesses potent inhibitory activity against Trypanosoma cruzi epimastigotes (IC50 = 4.1 µM)—the causative parasite of Chagas disease—was successfully achieved. Moreover, the cyclization strategy developed in this study facilitated the synthesis of noncanonical ...
Zhang J, Nakamura H.
europepmc   +3 more sources

Quinol derivatives as potential trypanocidal agents.

Bioorg Med Chem, 2012
Quinols have been developed as a class of potential anti-cancer compounds. They are thought to act as double Michael acceptors, forming two covalent bonds to their target protein(s). Quinols have also been shown to have activity against the parasite Trypanosoma brucei, the causative organism of human African trypanosomiasis, but they demonstrated ...
Capes A, Patterson S, Wyllie S, Hallyburton I, Collie IT, McCarroll AJ, Stevens MF, Frearson JA, Wyatt PG, Fairlamb AH, Gilbert IH.   +10 more
europepmc   +4 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

Preclinical data do not support the use of amiodarone or dronedarone as antiparasitic drugs for Chagas disease at the approved human dosing regimen

Frontiers in Tropical Diseases, 2023
The repurposing of approved drugs is an appealing method to fast-track the development of novel therapies for neglected diseases. Amiodarone and dronedarone, two approved antiarrhythmic agents, have been reported to have potential for the management of ...
Amanda F. Francisco, Gong Chen, Wen Wang, Melissa L. Sykes, Fanny Escudié, Ivan Scandale, Francisco Olmo, David M. Shackleford, Bilal Zulfiqar, Jadel M. Kratz, Thao Pham, Jessica Saunders, Meiyu Hu, Vicky M. Avery, Susan A. Charman, John M. Kelly, Eric Chatelain   +16 more
doaj   +1 more source

Lipophilic Guanylhydrazone Analogues as Promising Trypanocidal Agents: An Extended SAR Study [PDF]

Current Pharmaceutical Design, 2020
In this report, we extend the SAR analysis of a number of lipophilic guanylhydrazone analogues with respect to in vitro growth inhibition of Trypanosoma brucei and Trypanosoma cruzi. Sleeping sickness and Chagas disease, caused by the tropical parasites T. brucei and T.
Vasiliki Pardali, Erofili Giannakopoulou, Dimitrios-Ilias Balourdas, Vassilios Myrianthopoulos, Martin C. Taylor, Marina Šekutor, Kata Mlinarić-Majerski, John M. Kelly, Grigoris Zoidis   +8 more
openaire   +3 more sources

Anti-protozoal activity and metabolomic analyses of Cichorium intybus L. against Trypanosoma cruzi

International Journal for Parasitology: Drugs and Drug Resistance, 2022
Chagas disease, caused by the protozoa Trypanosoma cruzi, is a potentially life-threatening parasitic zoonosis infecting 6–7 million people worldwide, mainly in Latin America.
Miguel Peña-Espinoza, Yeambell Romero-Uzqueda, Angela H. Valente, Matthew de Roode, Henrik T. Simonsen, Stig M. Thamsborg, Andrew R. Williams, Rodrigo López-Muñoz   +7 more
doaj   +1 more source

New Lipophilic Hydroxamates as Promising Trypanocidal Agents: Design, Synthesis, SAR, and Conformational Behavior Studies. [PDF]

ACS Med Chem Lett
A series of novel hydroxamic acid derivatives was designed and synthesized, and their growth inhibitory activity against bloodstream form Trypanosoma brucei was evaluated. These compounds are based on conformationally constrained, lipophilic, spiro carbocyclic 2,6-diketopiperazine (2,6-DKP) scaffolds and bear a side pharmacophoric functionality that ...
Fytas G, Zoidis G, Drakopoulos A, Taylor MC, Kelly JM, Tsatsaroni A, Tsotinis A.   +6 more
europepmc   +4 more sources

Pilot-Scale Compound Screening against RNA Editing Identifies Trypanocidal Agents [PDF]

SLAS Discovery, 2015
Most mitochondrial messenger RNAs in trypanosomatid pathogens undergo a unique type of posttranscriptional modification involving insertion and/or deletion of uridylates. This process, RNA editing, is catalyzed by a multiprotein complex (~1.6 MDa), the editosome.
Houtan, Moshiri, Vaibhav, Mehta, Chun Wai, Yip, Reza, Salavati   +3 more
openaire   +2 more sources