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

Authors
  • Lachhab, Saida;
  • El Mansouri, Az-eddine;
  • Mehdi, Ahmad;
  • Dennemont, Indira;
  • Neyts, Johan; 14425;
  • Jochmans, Dirk; 15412;
  • Andrei, Graciela; 3409;
  • Snoeck, Robert; 12760;
  • Sanghvi, Yogesh S;
  • Ali, Mustapha Ait;
  • Loiseau, Philippe M;
  • Lazrek, Hassan B;
Publication Date
Oct 01, 2023
Source
Lirias
Keywords
License
Unknown
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Abstract

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 IC50 value at 8.98 µM on L. donovani intramacrophage amastigotes and a moderate selectivity index value at 2.4. / status: published

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