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Cytotoxicity and Leishmanicidal Activity of Isoniazid-Derived Hydrazones and 2-Pyrazineformamide Thiosemicarbazones
- Source :
- Journal of the Brazilian Chemical Society, Volume: 27, Issue: 4, Pages: 769-777, Published: APR 2016, Journal of the Brazilian Chemical Society v.27 n.4 2016, Journal of the Brazilian Chemical Society, Sociedade Brasileira de Química (SBQ), instacron:SBQ
- Publication Year :
- 2015
- Publisher :
- Sociedade Brasileira de Quimica (SBQ), 2015.
-
Abstract
- The isoniazid-derived hydrazones 2-pyridinecarbaldehyde- (HPCIH), 2-acetylpyridine- (HAPIH), 2-benzoylpyridine- (HBPIH), 2-pyridineformamide- (HPAmIH) and 2-pyrazineformamide- (HPzAmIH) isonicotinoyl hydrazones, as well as the pyrazinamide-derived thiosemicarbazones 2-pyrazineformamide- (HPzAm4DH), N(4)-methyl-2-pyrazineformamide- (HPzAm4M), N(4)-ethyl-2-pyrazineformamide- (HPzAm4E) and N(4)-phenyl-2-pyrazineformamide- (HPzAm4Ph) thiosemicarbazones, were assayed for their action against intracellular amastigote form of Leishmania (Viannia) braziliensis strains and the glioblastoma multiforme (SF-295), colon adenocarcinoma (HCT-116), ovarian cancer (OVCAR-8) and acute myeloid leukemia (HL-60) human tumor cell lines. All compounds exhibited leishmanicidal effects, with concentrations at which 50% of parasites were inhibited (IC50) in the 10.70-18.84 µM range. Moreover, the compounds were up to 30-fold less toxic to macrophages than to the parasites. Pyrazinamide-derived thiosemicarbazones proved to have poor activity against the tumor cell lines at 5 µg mL-1, whereas, in general the isoniazid-derived hydrazones presented good activity, being HAPIH and HBPIH the most potent compounds (IC50 = 0.42-1.5 µM).
- Subjects :
- chemistry.chemical_classification
isoniazid
biology
Stereochemistry
Isoniazid
Hydrazone
Myeloid leukemia
General Chemistry
Leishmania
biology.organism_classification
Molecular biology
thiosemicarbazone
chemistry.chemical_compound
hydrazone
chemistry
medicine
cytotoxicity
antileishmanial activity
Cytotoxicity
Amastigote
Semicarbazone
IC50
medicine.drug
Subjects
Details
- ISSN :
- 01035053
- Database :
- OpenAIRE
- Journal :
- Journal of the Brazilian Chemical Society
- Accession number :
- edsair.doi.dedup.....b74f385ea9fd7efb3f3c8a8d48fc6d35