Synthesis of new 3-acetyl-1,3,4-oxadiazolines combined with pyrimidines as antileishmanial and antiviral agents

A new series of 3-acetyl-1,3,4-oxadiazoline hybrid molecules was designed and synthesized using a condensation between acyclonucleosides and substituted phenylhydrazone. All intermediates and final products were screened against Leishmania donovani, a Protozoan parasite and against three viruses SAR...

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Detalles Bibliográficos
Autores principales: Lachhab, Saida, El Mansouri, Az-eddine, Mehdi, Ahmad, Dennemont, Indira, Neyts, Johan, Jochmans, Dirk, Andrei, Graciela, Snoeck, Robert, Sanghvi, Yogesh S., Ait Ali, Mustapha, Loiseau, Philippe M., Lazrek, Hassan B.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2022
Materias:
Original Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9573813/
https://www.ncbi.nlm.nih.gov/pubmed/36251201
http://dx.doi.org/10.1007/s11030-022-10548-9
Descripción
Sumario:A new series of 3-acetyl-1,3,4-oxadiazoline hybrid molecules was designed and synthesized using a condensation between acyclonucleosides and substituted phenylhydrazone. All intermediates and final products were screened against Leishmania donovani, a Protozoan parasite and against three viruses SARS-CoV-2, HCMV and VZV. While no significant activity was observed against the viruses, the intermediate with 6-azatymine as thymine and 5-azathymine-3-acetyl-1,3,4-oxadiazoline hybrid exhibited a significant antileishmanial activity. The later compound was the most promising, exhibiting an IC(50) value at 8.98 µM on L. donovani intramacrophage amastigotes and a moderate selectivity index value at 2.4. GRAPHICAL ABSTRACT: [Image: see text] SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s11030-022-10548-9.

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