Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents

ABSTRACT Introduction: Schistosomiasis is an infectious parasitic disease caused by trematodes of the genus Schistosoma, which threatens at least 258 million people worldwide and its control is dependent on a single drug, praziquantel. The aim of this study was to evaluate the anti-Schistosoma mansoni activity in vitro of novel imidazolidine derivatives. Material and methods: We synthesized two novel imidazolidine derivatives: (LPSF/PTS10) (Z)-1-(2-chloro-6-fluorobenzyl)-4-(4-dimethylaminobenzylidene)-5-thioxoimidazolidin-2-one and (LPSF/PTS23) (Z)-1-(2-chloro-6-fluoro-benzyl)-5-thioxo-4-(2,4,6-trimethoxy-benzylidene)-imidazolidin-2-one. The structures of two compounds were determined by spectroscopic methods. During the biological assays, parameters such as motility, oviposition, mortality and analysis by Scanning Electron Microscopy were performed. Results: LPSF/PTS10 and LPSF/PTS23 were considered to be active in the separation of coupled pairs, mortality and to decrease the motor activity. In addition, LPSF/PTS23 induced ultrastructural alterations in worms, after 24 h of contact, causing extensive erosion over the entire body of the worms. Conclusion: The imidazolidine derivatives containing the trimetoxy and benzylidene halogens showed promising in vitro schistosomicidal activity.

Microscopical study of the safety and toxicity of niclosamide as topical anti-schistosomal agent

In this study, 1% niclosamide lotion was tested for safety and toxicity on some vital organs of albino rats by applying 1 ml of the 1% niclosamide lotion on 1 x 1 inch to the skin every other day in total 3 times per week for 1 and 6 weeks [groups I and II]. The placebo was applied to the skin in the same way [groups III and IV]. The last group served as control non-treated one. Microscopically, the liver, kidney, heart and skin revealed normal cellular structures with no significant abnormalities in any of the treated groups. Also, the study showed that topical niclosamide is free from any serious histopathological effects when applied to the skin of rats

Study of safety and toxicity of niclosamide as a topical anti schistosomal agent

In this study, topical Niclosamide was tested for safety and toxicological, hematological and biochemical parameters. Fifty albino rats [25 males and 25 females] weighing between 140 to 180 grams were used. 1% lotion was used for painting the tail and the abdomen of rats three times weekly for one week in case of acute toxicity study and for 6 weeks in case of chronic toxicity. Animals in all groups were tested for allergic reactions, body weight, food consumption, activity and mortality. Hematological tests were performed, including liver function tests SGPT and SGOT, albumin and globulin and A/G ratio, kidney function tests as serum creatinine and urea were also carried out together with cholesterol level. The results revealed that topical Niclosamide is free from any serious toxicological effects