Eur J Med Chem. 2014 Aug 15;86C:17-30. doi: 10.1016/j.ejmech.2014.08.046. [Epub ahead of print]
D'Ascenzio M1, Bizzarri B2, De Monte C1, Carradori S1, Bolasco A1, Secci D1, Rivanera D3, Faulhaber N4, Bordón C4, Jones-Brando L4.
We designed and synthesized a large number of novel thiazolidin-4-one derivatives for the evaluation of their anti-Toxoplasma gondii activity. This scaffold was functionalized at the N1-hydrazine portion with aliphatic, cycloaliphatic and (hetero)aromatic moieties. Then, a benzyl pendant was introduced at the lactamic NH of the core nucleus to evaluate the influence of this chemical modification on biological activity. The compounds were subjected to several in vitro assays to assess their anti-parasitic efficacy, cytotoxicity on fibroblasts, inhibition of tachyzoite invasion/attachment and replication after treatment. Results showed that fourteen of these thiazole-based compounds compare favorably to control compound trimethoprim in terms of parasite growth inhibition.
Copyright © 2014. Published by Elsevier Masson SAS.
Copyright © 2014. Published by Elsevier Masson SAS.
KEYWORDS:
Cytotoxicity; Host cell invasion; Parasite growth inhibition; Thiazolidin-4-one; Toxoplasma- PMID:
- 25140751
- [PubMed - as supplied by publisher]
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