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Antischistosomal action of thioxo-imidazolidine compounds: an ultrastructural and cytotoxicity study.
- Source :
-
Experimental parasitology [Exp Parasitol] 2011 May; Vol. 128 (1), pp. 82-90. Date of Electronic Publication: 2011 Feb 16. - Publication Year :
- 2011
-
Abstract
- Schistosomiasis is a disease caused by helminthes of the genus Schistosoma, which threatens approximately 207 million people worldwide. Recently, strains of Schistosoma mansoni appear to be developing tolerance and resistance against Praziquantel, the most commonly available drug on the market used in the treatment of disease. This worrisome development justifies studies that seek alternatives for the prevention, treatment and cure of this disease. This study aimed to evaluate the in vitro activity of new imidazolidine compounds 1-benzyl-4-[(4-chloro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-5) and 1-(4-chloro-benzyl)-4-[(4-fluoro-phenyl)-hydrazono]-5-thioxo-imidazolidin-2-one (LPSF/PT-11) against adult worms of S. mansoni. LPSF/PT-5 and LPSF/PT-11 imidazolidine derivatives showed relevant schistosomicidal activity in vitro and induced significant ultrastructural alterations in worms and cell death: results similar to praziquantel. Thus, it is possible that these imidazolidine derivatives can be future candidates as schistosomotic drugs, but further studies are needed to elucidate the induced mechanisms behind this response.<br /> (Copyright © 2011 Elsevier Inc. All rights reserved.)
- Subjects :
- Animals
Annexin A5 chemistry
Apoptosis drug effects
Biomphalaria
Cell Survival drug effects
Enzyme Inhibitors chemistry
Female
Fluorescein-5-isothiocyanate chemistry
Fluorescent Dyes chemistry
Imidazolidines toxicity
Indicators and Reagents chemistry
Male
Mice
Mice, Inbred BALB C
Microscopy, Electron, Scanning
Necrosis
Praziquantel pharmacology
Praziquantel toxicity
Propidium chemistry
Schistosoma mansoni ultrastructure
Schistosomiasis mansoni drug therapy
Schistosomicides toxicity
Spleen cytology
Spleen drug effects
Spleen pathology
Imidazolidines pharmacology
Schistosoma mansoni drug effects
Schistosomiasis mansoni parasitology
Schistosomicides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2449
- Volume :
- 128
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Experimental parasitology
- Publication Type :
- Academic Journal
- Accession number :
- 21315071
- Full Text :
- https://doi.org/10.1016/j.exppara.2011.01.021