Antiplasmodial, Trypanocidal, and Genotoxicity
antiparasitic activity
atorvastatin
chemical synthesis
drug development
genotoxicity assessment
hybrid compounds
phenylacetamides
Journal
Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453
Informations de publication
Date de publication:
24 May 2023
24 May 2023
Historique:
received:
16
04
2023
revised:
13
05
2023
accepted:
19
05
2023
medline:
28
6
2023
pubmed:
28
6
2023
entrez:
28
6
2023
Statut:
epublish
Résumé
Statins present a plethora of pleiotropic effects including anti-inflammatory and antimicrobial responses. A,α-difluorophenylacetamides, analogs of diclofenac, are potent pre-clinical anti-inflammatory non-steroidal drugs. Molecular hybridization based on the combination of pharmacophoric moieties has emerged as a strategy for the development of new candidates aiming to obtain multitarget ligands. Considering the anti-inflammatory activity of phenylacetamides and the potential microbicidal action of statins against obligate intracellular parasites, the objective of this work was to synthesize eight new hybrid compounds of α,α-difluorophenylacetamides with the moiety of statins and assess their phenotypic activity against None of the sodium salt compounds presented antiparasitic activity and two acetated compounds displayed mild anti- However, the chlorinated derivative was the most promising compound with chemical and biological profitable characteristics, without presenting genotoxicity
Sections du résumé
BACKGROUND
BACKGROUND
Statins present a plethora of pleiotropic effects including anti-inflammatory and antimicrobial responses. A,α-difluorophenylacetamides, analogs of diclofenac, are potent pre-clinical anti-inflammatory non-steroidal drugs. Molecular hybridization based on the combination of pharmacophoric moieties has emerged as a strategy for the development of new candidates aiming to obtain multitarget ligands.
METHODS
METHODS
Considering the anti-inflammatory activity of phenylacetamides and the potential microbicidal action of statins against obligate intracellular parasites, the objective of this work was to synthesize eight new hybrid compounds of α,α-difluorophenylacetamides with the moiety of statins and assess their phenotypic activity against
RESULTS
RESULTS
None of the sodium salt compounds presented antiparasitic activity and two acetated compounds displayed mild anti-
CONCLUSIONS
CONCLUSIONS
However, the chlorinated derivative was the most promising compound with chemical and biological profitable characteristics, without presenting genotoxicity
Identifiants
pubmed: 37375730
pii: ph16060782
doi: 10.3390/ph16060782
pmc: PMC10301432
pii:
doi:
Types de publication
Journal Article
Langues
eng
Subventions
Organisme : Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
ID : E-26/202.805/2017
Organisme : Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
ID : E-26/200.839/2021
Organisme : Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
ID : E-26/010.002119/2019
Organisme : Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
ID : E-26/010.100956/2018
Organisme : Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
ID : E-26/210.096/2023
Organisme : Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
ID : E-26/200.825/2021
Organisme : Fundação Carlos Chagas Filho de Amparo à Pesquisa do Estado do Rio de Janeiro
ID : E-26/202.925/2017
Organisme : National Council for Scientific and Technological Development
ID : 302345/2017-5
Organisme : National Council for Scientific and Technological Development
ID : 306193/2018-3
Organisme : National Council for Scientific and Technological Development
ID : 302160/2019
Organisme : Coordenação de Aperfeicoamento de Pessoal de Nível Superior
ID : 0001
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