Biological Evaluation and X‐ray Co‐crystal Structures of Cyclohexylpyrrolidine Ligands for Trypanothione Reductase, an Enzyme from the Redox Metabolism of Trypanosoma
Sign Up to like & getrecommendations! Published in 2018 at "ChemMedChem"
DOI: 10.1002/cmdc.201800067
Abstract: The tropical diseases human African trypanosomiasis, Chagas disease, and the various forms of leishmaniasis are caused by parasites of the family of trypanosomatids. These protozoa possess a unique redox metabolism based on trypanothione and trypanothione… read more here.
Keywords: reductase; crystal structures; ray crystal; trypanothione reductase ... See more keywords
Febrifugine analogues as Leishmania donovani trypanothione reductase inhibitors: binding energy analysis assisted by molecular docking, ADMET and molecular dynamics simulation
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2015.1135298
Abstract: Visceral leishmaniasis affects people from 70 countries worldwide, mostly from Indian, African and south American continent. The increasing resistance to antimonial, miltefosine and frequent toxicity of amphotericin B drives an urgent need to develop an… read more here.
Keywords: molecular dynamics; febrifugine analogues; leishmania donovani; trypanothione reductase ... See more keywords
Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2016.1250755
Abstract: Abstract The study presented here aimed at identifying a new class of compounds acting against Leishmania parasites, the causative agent of Leishmaniasis. For this purpose, the thioether derivatives of our in-house library have been evaluated… read more here.
Keywords: trypanothione; inhibition leishmania; leishmania infantum; trypanothione reductase ... See more keywords
Cyclobenzaprine Raises ROS Levels in Leishmania infantum and Reduces Parasite Burden in Infected Mice
Sign Up to like & getrecommendations! Published in 2017 at "PLoS Neglected Tropical Diseases"
DOI: 10.1371/journal.pntd.0005281
Abstract: Background The leishmanicidal action of tricyclic antidepressants has been studied and evidences have pointed that their action is linked to inhibition of trypanothione reductase, a key enzyme in the redox metabolism of pathogenic trypanosomes. Cyclobenzaprine… read more here.
Keywords: cbp; infantum infected; infected mice; trypanothione reductase ... See more keywords
Innovative Approach for a Classic Target: Fragment Screening on Trypanothione Reductase Reveals New Opportunities for Drug Design
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Molecular Biosciences"
DOI: 10.3389/fmolb.2022.900882
Abstract: Trypanothione reductase (TR) is a key factor in the redox homeostasis of trypanosomatid parasites, critical for survival in the hostile oxidative environment generated by the host to fight infection. TR is considered an attractive target… read more here.
Keywords: design; site; trypanothione; target ... See more keywords
Identification of 3-Methoxycarpachromene and Masticadienonic Acid as New Target Inhibitors against Trypanothione Reductase from Leishmania Infantum Using Molecular Docking and ADMET Prediction
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DOI: 10.3390/molecules26113335
Abstract: Polyphenolic and Terpenoids are potent natural antiparasitic compounds. This study aimed to identify new drug against Leishmania parasites, leishmaniasis’s causal agent. A new in silico analysis was accomplished using molecular docking, with the Autodock vina… read more here.
Keywords: trypanothione reductase; using molecular; masticadienonic acid; methoxycarpachromene masticadienonic ... See more keywords
New Amino Naphthoquinone Derivatives as Anti-Trypanosoma cruzi Agents Targeting Trypanothione Reductase
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DOI: 10.3390/pharmaceutics14061121
Abstract: 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 vitro on the epimastigote and trypomastigote forms of Trypanosoma… read more here.
Keywords: naphthoquinone; trypanosoma cruzi; naphthoquinone derivatives; trypanothione reductase ... See more keywords