Activity of 9-acridanone-hydrazone drugs detected at the pre-postural phase, in the experimental schistosomiasis mansoni

Pereira, Leandro de Mattos; Coelho, Paulo Marcos Zech; Costa, J. O.; Mello, Rodrigo Fernandes de

doi:10.1590/s0074-02761995000300021

Cited by 21 publications

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“…In another study, 9-acridanones derived from thiazoles were effective against S. mansoni in the skin phase, killing almost all of the parasites in mice at a dose of 100 mg/kg, 24 h after penetration by cercariae. This same study showed that when the compound is administered to monkeys at a dose of 25 mg/kg, worms and eggs are absent from liver tissue and rectal mucosa 7 days after infection, which constitutes cure (20).…”

Section: Discussionmentioning

confidence: 83%

“…It is well known that hydrazones, thiosemicarbazones, and phthalimides as well as thiazoles are considered privileged structures as leads in medicinal chemistry (19)(20)(21). These core structures have figured prominently in a vast number of structural subunits used for a broad spectrum of activities, and the mode of action of the nuclei of these pharmacophores is usually attributed to the inhibition of multiple targets.…”

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confidence: 99%

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Evaluation of the Anti-Schistosoma mansoni Activity of Thiosemicarbazones and Thiazoles

Santiago

Oliveira

Filho

et al. 2014

Antimicrob Agents Chemother

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f Schistosomiasis is a chronic and debilitating disease caused by a trematode of the genus Schistosoma and affects over 207 million people. Chemotherapy is the only immediate recourse for minimizing the prevalence of this disease and involves predominately the administration of a single drug, praziquantel (PZQ). Although PZQ has proven efficacy, there is a recognized need to develop new drugs as schistosomicides since studies have shown that repeated use of this drug in areas of endemicity may cause a temporary reduction in susceptibility in isolates of Schistosoma mansoni. Hydrazones, thiosemicarbazones, phthalimides, and thiazoles are thus regarded as privileged structures used for a broad spectrum of activities and are potential candidates for sources of new drug prototypes. The present study determined the in vitro schistosomicidal activity of 10 molecules containing these structures. During the assays, parameters such motility and mortality, oviposition, morphological changes in the tegument, cytotoxicity, and immunomodulatory activity caused by these compounds were evaluated. The results showed that compounds formed of thiazole and phthalimide led to higher mortality of worms, with a significant decline in motility, inhibition of pairing and oviposition, and a mortality rate of 100% starting from 144 h of exposure. These compounds also stimulated the production of nitric oxide and tumor necrosis factor alpha (TNF-␣), thereby demonstrating the presence of immunomodulatory activity. The phthalyl thiazole LpQM-45 caused significant ultrastructural alterations, with destruction of the tegument in both male and female worms. According to the present study, phthalyl thiazole compounds possess antischistosomal activities and should form the basis for future experimental and clinical trials.

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Section: Discussionmentioning

confidence: 83%

mentioning

confidence: 99%

Evaluation of the Anti-Schistosoma mansoni Activity of Thiosemicarbazones and Thiazoles

Santiago

Oliveira

Filho

et al. 2014

Antimicrob Agents Chemother

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“…In addition, same compounds were found to be effective against S. mansoni in mice, killing almost all the skin schistosomules, when administered at the dose of 100mg/kg. In experiments carried out with Cebus monkeys, the compound RO 15-5458 / 000 was shown to be fully effective at 25 mg/kg [76].…”

Section: Schistosomiasismentioning

confidence: 99%

Biological Activities of Hydrazone Derivatives

2007

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There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH-proton constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

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“…In experiments carried out with Cebus monkeys, the compound RO 15-5458 / 000 was shown to be fully effective at 25 mg/kg. 33 …”

Section: Antischistosomiasismentioning

confidence: 99%

Biological Activities of Hydrazone Derivatives in the New Millennium

Negi¹

2013

Int J Pharmceut Chem

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ABSTRACT:Hydrazones are present in many of the bioactive heterocyclic compounds that are of wide interest because of their diverse biological and clinical applications. This created interest in researchers who have synthesized variety of hydrazone derivatives and screened them for their various biological activities viz. anticonvulsant, antidepressant, analgesic, anti-inflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, anticancer, vasodialator, antiviral, antischistosomiasis, anti-HIV, anthelmintic, antidiabetic and trypanocidal activities. Hydrazones possessing an azometine -NHN=CH-proton constitute an important class of compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

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Activity of 9-acridanone-hydrazone drugs detected at the pre-postural phase, in the experimental schistosomiasis mansoni

Cited by 21 publications

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Evaluation of the Anti-Schistosoma mansoni Activity of Thiosemicarbazones and Thiazoles

Evaluation of the Anti-Schistosoma mansoni Activity of Thiosemicarbazones and Thiazoles

Biological Activities of Hydrazone Derivatives

Biological Activities of Hydrazone Derivatives in the New Millennium

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