Biological activities of 4H-thiochromen-4-one 1,1-dioxide derivatives against tropical disease parasites: A target-based drug design approach.
Allosteric inhibition
Bioisosteric replacements
Reactive oxygen species
Tropical diseases
Trypanothione reductase
Journal
Heliyon
ISSN: 2405-8440
Titre abrégé: Heliyon
Pays: England
ID NLM: 101672560
Informations de publication
Date de publication:
Jul 2023
Jul 2023
Historique:
received:
05
03
2023
revised:
12
06
2023
accepted:
28
06
2023
medline:
24
7
2023
pubmed:
24
7
2023
entrez:
24
7
2023
Statut:
epublish
Résumé
A promising strategy for developing novel therapies against tropical diseases, including malaria, leishmaniasis, and trypanosomiasis, is to detect biological targets such as trypanothione reductase, a vital parasite enzyme that regulates oxidative stress. This enzyme is highly selective and conserved in the Trypanosotidae family and has an ortholog in the Plasmodium genus. Previous studies have established that an isosteric replacement of naphthoquinone's carbonyl group with a sulfone group leads to compounds with high bioactivity and selectivity (half-maximal inhibitory concentration = 3 μM against intracellular amastigotes of
Identifiants
pubmed: 37483711
doi: 10.1016/j.heliyon.2023.e17801
pii: S2405-8440(23)05009-0
pmc: PMC10362183
doi:
Types de publication
Journal Article
Langues
eng
Pagination
e17801Informations de copyright
© 2023 The Authors.
Déclaration de conflit d'intérêts
The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper
Références
J Chem Inf Model. 2021 Aug 23;61(8):3891-3898
pubmed: 34278794
Biochem Pharmacol. 2010 Jun 15;79(12):1736-45
pubmed: 20178775
J Chem Theory Comput. 2005 Sep;1(5):900-7
pubmed: 26641906
Molecules. 2020 Feb 12;25(4):
pubmed: 32059518
Molecules. 2017 Nov 29;22(12):
pubmed: 29186046
Drug Target Insights. 2007;2:129-46
pubmed: 21901070
Int J Parasitol Drugs Drug Resist. 2020 Aug;13:94-106
pubmed: 32734890
J Comput Chem. 2011 Jul 30;32(10):2149-59
pubmed: 21541955
J Med Chem. 2010 Nov 25;53(22):7902-17
pubmed: 20804202
ChemMedChem. 2013 Jul;8(7):1175-83
pubmed: 23733388
FEBS Lett. 2020 May;594(9):1403-1412
pubmed: 31981230
Antimicrob Agents Chemother. 1996 Nov;40(11):2592-7
pubmed: 8913471
J Med Chem. 1997 Jul 18;40(15):2314-22
pubmed: 9240347
Nucleic Acids Res. 2011 Jul;39(Web Server issue):W270-7
pubmed: 21624888
J Comput Chem. 2010 Jan 30;31(2):455-61
pubmed: 19499576
Parasitol Res. 2012 Jan;110(1):341-8
pubmed: 21717278
Acta Trop. 2012 Apr;122(1):36-45
pubmed: 22155571
J Am Chem Soc. 2006 Aug 23;128(33):10784-94
pubmed: 16910673
Am J Trop Med Hyg. 2007 Jun;76(6):1107-12
pubmed: 17556619