Semisynthetic and newly designed derivatives based on natural chemical scaffolds: moving beyond natural products to fight Trypanosoma cruzi
R da Rosa, EP Schenkel, LS Campos Bernardes - Phytochemistry reviews, 2020 - Springer
… The use of natural products as chemical scaffolds or starting materials to obtain novel compounds
… cruzi. We highlight the chemical modifications that might influence their bioactivity and …
… cruzi. We highlight the chemical modifications that might influence their bioactivity and …
[HTML][HTML] Identification of novel chemical scaffolds inhibiting trypanothione synthetase from pathogenic trypanosomatids
…, T Calogeropoulou, A Detsi, T Jaeger… - PLoS neglected …, 2016 - journals.plos.org
… three major pathogen species (Trypanosoma brucei, Trypanosoma cruzi and Leishmania
infantum)… Several novel chemical scaffolds were identified as low μM and selective tri-tryp TryS …
infantum)… Several novel chemical scaffolds were identified as low μM and selective tri-tryp TryS …
[HTML][HTML] Novel scaffolds for inhibition of Cruzipain identified from high-throughput screening of anti-kinetoplastid chemical boxes
E Salas-Sarduy, LU Landaburu, J Karpiak… - Scientific reports, 2017 - nature.com
… or Chagas disease is a prevalent, neglected and serious debilitating illness caused by the
kinetoplastid protozoan parasite Trypanosoma cruzi. The current chemotherapy is limited only …
kinetoplastid protozoan parasite Trypanosoma cruzi. The current chemotherapy is limited only …
Facing Chagas' Disease: Trypanocidal Properties of New Coumarinchalcone Scaffolds
S Vazquez-Rodriguez, RF Guinez… - … Chemistry, 2016 - ingentaconnect.com
… chemical entities based on coumarin and chalcone scaffolds, … stages of the Trypanosoma
cruzi parasite. Cytotoxicity assays … 2 and 5 in the designed scaffold seemed to be a key feature …
cruzi parasite. Cytotoxicity assays … 2 and 5 in the designed scaffold seemed to be a key feature …
[HTML][HTML] Bioactivity of Novel Pyrazole-Thiazolines Scaffolds against Trypanosoma cruzi: Computational Approaches and 3D Spheroid Model on Drug Discovery for …
LS Lara, GC Lechuga, LMR Orlando, BS Ferreira… - Pharmaceutics, 2022 - mdpi.com
… the development of new chemical entities with potent activity against Trypanosoma cruzi, are
a … This new scaffold will be targeted to optimize in order to enhance its biological activity to …
a … This new scaffold will be targeted to optimize in order to enhance its biological activity to …
Potent inhibitor scaffold against Trypanosoma cruzi trans-sialidase
S Arioka, M Sakagami, R Uematsu… - … & medicinal chemistry, 2010 - Elsevier
… cruzi trans-sialidase (TcTS). However, inhibitors found to date are not strong enough to serve
as a lead scaffold… These compounds may serve as potent lead chemotherapeutic scaffolds …
as a lead scaffold… These compounds may serve as potent lead chemotherapeutic scaffolds …
Triazole-containing heterocycles: Privileged scaffolds in anti-Trypanosoma cruzi drug development
KB Pone, S Dalhatou, HK Paumo… - Current Drug …, 2022 - ingentaconnect.com
Background: Chagas disease is a potentially life-threatening illness caused by the protozoan
parasite Trypanosoma cruzi and is transmitted to humans through the excreta of infected …
parasite Trypanosoma cruzi and is transmitted to humans through the excreta of infected …
Cruzipain: an update on its potential as chemotherapy target against the human pathogen Trypanosoma cruzi
MH Branquinha, SSC Oliveira… - … medicinal chemistry, 2015 - ingentaconnect.com
… of a specific SAR using high speed chemistry, three-dimensional enzyme structure guided
… to lengthen the diversity of chemical scaffolds available for developing cruzipain inhibitors. …
… to lengthen the diversity of chemical scaffolds available for developing cruzipain inhibitors. …
Synthesis and biological evaluation of isoxazolyl-sulfonamides: A non-cytotoxic scaffold active against Trypanosoma cruzi, Leishmania amazonensis and Herpes …
… Our results have shown that the isoxazolyl-sulfonamide scaffold is promising regarding
all biological activities studied herein, especially the inhibitory activity against T. cruzi. …
all biological activities studied herein, especially the inhibitory activity against T. cruzi. …
Hydroxamic acid derivatives: a promising scaffold for rational compound optimization in Chagas disease
DR de Menezes, CM Calvet… - … Medicinal Chemistry, 2016 - Taylor & Francis
… Ultrastructural alterations after treatment of cardiomyocytes or macrophages infected by
Trypanosoma cruzi with the IC 50 value of HAD1 revealed alterations to amastigotes, showing …
Trypanosoma cruzi with the IC 50 value of HAD1 revealed alterations to amastigotes, showing …
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