Results 11 to 20 of about 7,490 (202)

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
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
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In Silico Studies and Biological Evaluation of Thiosemicarbazones as Cruzain-Targeting Trypanocidal Agents for Chagas Disease [PDF]

Pharmaceutics
Background/Objectives: Chagas disease remains a major unmet medical need due to the limited efficacy and safety of current therapies. Here, we investigated sixteen thiosemicarbazone (TSC) derivatives as cruzain inhibitors using an integrated in silico/in
Lidiane Meier, Milena F. C. V. de Melo, Heitor R. Abreu, Isabella M. e Oliveira, Larissa Sens, Thiago H. Doring, Renata Krogh, Adilson Beatriz, Adriano D. Andricopulo, Sumbal Saba, Aldo S. de Oliveira, Jamal Rafique   +11 more
doaj   +2 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

Mechanistic Exploration of N,N′-Disubstituted Diamines as Promising Chagas Disease Treatments [PDF]

Pharmaceuticals
Introduction: Chagas disease, caused by the protozoan Trypanosoma cruzi, remains a major public health concern due to the limited effectiveness of current treatments, especially in the chronic stage.
Alejandro I. Recio-Balsells, Chantal Reigada, María Gabriela Mediavilla, Esteban Panozzo-Zénere, Miguel Villarreal Parra, Patricia S. Doyle, Juan C. Engel, Claudio A. Pereira, Julia A. Cricco, Guillermo R. Labadie   +9 more
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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
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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

Prevention of congenital chagas disease by trypanocide treatment in women of reproductive age: A meta-analysis of observational studies. [PDF]

PLoS Neglected Tropical Diseases
BackgroundMaternal-foetal transmission of Chagas disease (CD) affects newborns worldwide. Although Benznidazole and Nifurtimox therapies are the standard treatments, their use during pregnancy is contra-indicated.
Francisco Cezar Aquino de Moraes, Maria Eduarda Cavalcanti Souza, Lucca Dal Moro, Isabelle Batista Donadon, Emanuele Rocha da Silva, Dilma do Socorro Moraes de Souza, Rommel Mario Rodríguez Burbano   +6 more
doaj   +2 more sources

In Silico Investigation of TATA-Binding Protein as a Therapeutic Target for Chagas Disease: Insights into FDA Drug Repositioning [PDF]

Pharmaceuticals
Background: Parasitic diseases, particularly Chagas disease caused by Trypanosoma cruzi, primarily affect developing countries but are now spreading to wealthier nations due to changing migration patterns. With approximately 8 to 9 million cases annually
Carlos Gaona-López, Domingo Méndez-Álvarez, Alonzo Gonzalez-Gonzalez, Guadalupe Avalos-Navarro, Alma D. Paz-González, Adriana Moreno-Rodríguez, Benjamín Nogueda-Torres, Gildardo Rivera   +7 more
doaj   +2 more sources

Synthesis and Biological Evaluation of Tetrahydroisoquinoline Derivatives as Trypanocidal Agents [PDF]

ACS Omega
João Paulo de Moura Lopes, Gabriel Vitor de Lima Marques, Lucas Abreu Diniz, Viviane Côrrea Santos, Daniela de Melo Resende, Silvane Maria Fonseca Murta, Markus Kohlhoff, Vinícius Gonçalves Maltarollo, Rafaela Salgado Ferreira, Renata Barbosa Oliveira   +9 more
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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