Synthesis and evaluation of the in vitro and in vivo antitrypanosomal activity of 2-styrylquinolines

R Espinosa, S Robledo, C Guzmán, N Arbeláez… - Heliyon, 2021 - cell.com
In this study, we report the synthesis and evaluation of in vitro and in vivo antitrypanosomal
activity of styrylquinoline-like compounds (SQ) 3a-h. Synthesis was carried out by using …

Orally active and selective tubulin inhibitors as anti-trypanosome agents

V Nanavaty, R Lama, R Sandhu, B Zhong, D Kulman… - PLoS …, 2016 - journals.plos.org
Objectives There is an urgent need to develop a safe, effective, orally active, and
inexpensive therapy for African trypanosomiasis due to the drawbacks of current drugs …

Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities

FVC e Mello, BMCS Quaresma, MCR Pitombeira… - European Journal of …, 2020 - Elsevier
The current treatment of Chagas disease is based on the use of two drugs, nifurtimox (Nfx)
and benznidazole (Bnz), both of which present limited efficacy in the chronic stage of the …

Synthesis and Evaluation of Quinone Derivatives for Activity against Trypanosome cruzi

Y Suto, T Ascencio, T Nobuta, N Yamagiwa… - Chemical and …, 2021 - jstage.jst.go.jp
A series of quinone derivatives with a variety of side chains were synthesized. These
synthetic quinone compounds were evaluated for in vitro antitrypanosomal activity against …

Synthesis and biological evaluation of imidamide analogs as selective anti-trypanosomal agents

V Bobba, Y Li, M Afrin, R Dano, W Zhang, B Li… - Bioorganic & medicinal …, 2022 - Elsevier
Human African trypanosomiasis is caused by a protozoan parasite Trypanosoma brucei
majorly infecting people living in sub-Saharan Africa. Current limited available treatments …

Trypanocidal properties, structure–activity relationship and computational studies of quinoxaline 1, 4-di-N-oxide derivatives

Y Estevez, M Quiliano, A Burguete, B Cabanillas… - Experimental …, 2011 - Elsevier
Pyrazole and propenone quinoxaline derivatives were tested against intracellular forms of
Leishmania peruviana and Trypanosoma cruzi. Both series were tested for toxicity against …

Synthesis and biological activity against Trypanosoma cruzi of substituted 1, 4-naphthoquinones

AO da Silva, R da Silva Lopes, RV de Lima… - European Journal of …, 2013 - Elsevier
The discovery and development of essential drugs for Chagas disease is a major concern
worldwide. New substituted 1, 4-naphthoquinones were synthesized and tested against the …

Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active …

F Palace-Berl, KFM Pasqualoto, B Zingales… - European Journal of …, 2018 - Elsevier
Chagas disease, caused by the protozoan Trypanosoma cruzi, is a neglected chronic
tropical infection endemic in Latin America. New and effective treatments are urgently …

New Amino Naphthoquinone Derivatives as Anti-Trypanosoma cruzi Agents Targeting Trypanothione Reductase

C Espinosa-Bustos, M Ortiz Pérez… - Pharmaceutics, 2022 - mdpi.com
To develop novel chemotherapeutic alternatives for the treatment of Chagas disease, in this
study, a set of new amino naphthoquinone derivatives were synthesised and evaluated in …

Pharmacological investigations on current and new drugs for treatment of human African trypanosomiasis

J Keiser - 1999 - edoc.unibas.ch
Trypanosomiasis remains a major threat to humans in sub-Saharan Africa with 55-60 million
people in 36 countries at risk of infection with Tb gambiense or Tb rhodesiense. Only a few …