Results 11 to 20 of about 5,661 (215)

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

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   +5 more sources

Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents [PDF]

Molecules, 2000
It describes the synthesis of new 1,2,6-Thiadiazin 1,1-dioxide derivatives using condensation of the Knoevenagel type. The products are evaluated in vitro as trypanocidal agents.
Hugo Cerecetto, Rossanna Di Maio, Gustavo Seoane, C. Ochoa, Alicia Gómez‐Barrio, Susana Muelas   +5 more
openalex   +4 more sources

Gossypol: a potential trypanocidal agent Gossypol: um agente potencialmente tripanocida

Revista da Sociedade Brasileira de Medicina Tropical, 1985
Antonio Blanco
doaj   +2 more sources

Synthesis of New Hybrid Derivatives from Metronidazole and Eugenol Analogues as Trypanocidal Agents

Journal of Pharmacy & Pharmaceutical Sciences, 2021
Background: The search for new drug compounds is always challenging and there are several different strategies that involve the most varied and creative approaches in medicinal chemistry. One of them is the technique of molecular hybridisation: forming a hybrid compound from two or more pharmacophoric subunits.
Mônica Fraccarolli Pelozo, Giovanna Fiori Serpa Lima, Cleydson Finotti Cordeiro, Luana Sueli Silva, Ivo Santana Caldas, Diogo Teixeira Carvalho, Stefânia Neiva Lavorato, Jamie Anthony Hawkes, Lucas Lopardi Franco   +8 more
openalex   +5 more sources

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

Bioorganic & Medicinal Chemistry Letters, 2016
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 ...
Heeren M. Gordhan, Stephen L. Patrick, Maria I. Swasy, Amber L. Hackler, Mark Anayee, Jennifer E. Golden, James C. Morris, Daniel C. Whitehead   +7 more
openalex   +3 more sources

Novel African Trypanocidal Agents: Membrane Rigidifying Peptides [PDF]

PLoS ONE, 2012
The bloodstream developmental forms of pathogenic African trypanosomes are uniquely susceptible to killing by small hydrophobic peptides. Trypanocidal activity is conferred by peptide hydrophobicity and charge distribution and results from increased rigidity of the plasma membrane. Structural analysis of lipid-associated peptide suggests a mechanism of
John M. Harrington, Chris L. Scelsi, Andreas Hartel, Nicola G. Jones, Markus Engstler, Paul Capewell, Annette MacLeod, Stephen L. Hajduk   +7 more
openalex   +6 more sources

Synthesis of indazol‐4,7‐dione derivatives as potential trypanocidal agents

Journal of Heterocyclic Chemistry, 2002
AbstractThe synthesis of new indazol‐4,7‐dione derivatives via 1,3‐dipolar cycloaddition of diazomethane with 2,3‐dimethyl‐1,4‐benzoquinone (2) and 1,4‐naphthoquinone (7) followed by N‐alkylation of the pyrazol nitrogen atom of the corresponding quinones (3) and (8) with methyl chloroacetate is described.
Ricardo A. Tapia, Claudia Carrasco, Scarlet Ojeda, Cristian O. Salas, Jaime A. Valderrama, Antonio Morello, Yolanda Repetto   +6 more
openalex   +6 more sources

Intravenous liposomal benznidazole as trypanocidal agent: increasing drug delivery to liver is not enough [PDF]

International Journal of Pharmaceutics, 2004
With the aim of investigating if delivery of benznidazole (BNZ) to liver could be increased by incorporating the drug in multilamellar liposomes, single bolus of free BNZ or liposomal BNZ formulations (MLV-BNZ) composed of HSPC:DSPG:Chol 2:1:2 (mol/mol/mol) at 0.7% (w/w) drug/total lipid ratio, were injected by intramuscular (i.m.), subcutaneous (s.c.)
María José Morilla, Jorge Montanari, María Jimena Prieto, M.O Lopez, Patricia B. Petray, Eder Lilia Romero   +5 more
openalex   +4 more sources

Huprines as a new family of dual acting trypanocidal–antiplasmodial agents [PDF]

Bioorganic & Medicinal Chemistry, 2011
A series of 19 huprines has been evaluated for their activity against cultured bloodstream forms of Trypanosoma brucei and Plasmodium falciparum. Moreover, cytotoxicity against rat myoblast L6 cells was assessed for selected huprines. All the tested huprines are moderately potent and selective trypanocidal agents, exhibiting IC(50) values against T ...
Julien Defaux, Marta Sala, X. Formosa, Carles Galdeano, Martin C. Taylor, Waleed A Alobaid, John M. Kelly, Colin W. Wright, Pelayo Camps, Diego Muñoz‐Torrero   +9 more
openalex   +6 more sources