Inhibition of
Leishmania infantum
NADPH binding site
X-ray crystal structure
cluster docking
procainamide derivatives
procaine derivatives
trypanothione reductase inhibition
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
01 Jan 2023
01 Jan 2023
Historique:
received:
14
11
2022
revised:
15
12
2022
accepted:
28
12
2022
entrez:
8
1
2023
pubmed:
9
1
2023
medline:
11
1
2023
Statut:
epublish
Résumé
As a result of the paucity of treatment, Leishmaniasis continues to provoke about 60,000 deaths every year worldwide. New molecules are needed, and drug discovery research is oriented toward targeting proteins crucial for parasite survival. Among them, trypanothione reductase (TR) is of remarkable interest owing to its vital role in We designed and synthesized new 3-amino-1-arylpropan-1-one derivatives structurally related to compound The newly synthesized compounds were screened at a concentration of 100 μM in in vitro assays and all of them proved to be active with residual activity percentages lower than 75%. Compounds
Sections du résumé
BACKGROUND
BACKGROUND
As a result of the paucity of treatment, Leishmaniasis continues to provoke about 60,000 deaths every year worldwide. New molecules are needed, and drug discovery research is oriented toward targeting proteins crucial for parasite survival. Among them, trypanothione reductase (TR) is of remarkable interest owing to its vital role in
METHODS
METHODS
We designed and synthesized new 3-amino-1-arylpropan-1-one derivatives structurally related to compound
RESULTS
RESULTS
The newly synthesized compounds were screened at a concentration of 100 μM in in vitro assays and all of them proved to be active with residual activity percentages lower than 75%.
CONCLUSIONS
CONCLUSIONS
Compounds
Identifiants
pubmed: 36615531
pii: molecules28010338
doi: 10.3390/molecules28010338
pmc: PMC9823735
pii:
doi:
Substances chimiques
trypanothione reductase
EC 1.8.1.12
NADP
53-59-8
NADH, NADPH Oxidoreductases
EC 1.6.-
Antiprotozoal Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Sapienza University of Rome
ID : Ateneo 2019 (RM11916B6AFDBEBD)
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