Interaction of Morphine With a New α2-Adrenoceptor Agonist in Mice

Sudo, Roberto T.; Calasans-Maia, Jorge A.; Galdino, Suely Lins; Lima, Maria Alice Gomes de Andrade; Zapata‐Sudo, Gisele; Hernandes, Marcelo Zaldini; Pitta, Ivan R.

doi:10.1016/j.jpain.2009.08.001

Cited by 31 publications

(34 citation statements)

References 45 publications

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“…In recent years, molecules containing indole-imidazolidine nuclei have been identified as promising drugs for the treatment of inflammation and pain [15,22]. In this work, we found that LPSF/NN-56 and LPSF/NN-52 derivatives exhibited promising anti-inflammatory and antinociceptive activities.…”

Section: Discussionmentioning

confidence: 69%

Anti-inflammatory and antinociceptive activities of indole–imidazolidine derivatives

Guerra

Malta

Laranjeira

et al. 2011

International Immunopharmacology

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Non-steroidal anti-inflammatory drugs (NSAIDs) represent a group of approximately 50 different medicines that are widely prescribed for the management of inflammation and that exhibit variable anti-inflammatory, anti-pyretic and analgesic activities. Most NSAIDs also exhibit a shared set of adverse effects, particularly related to gastrointestinal complications; thus, the development of new drugs for the treatment of chronic inflammation and pain continues to be an issue of high interest. Hydantoin and indole derivatives are reported to possess various pharmacological effects, including anti-inflammatory and analgesic activities. Therefore, the aim of this study was to evaluate the potential anti-inflammatory and antinociceptive activities of hybrid molecules containing imidazole and indole nuclei. The anti-inflammatory activities of 5-(1H-Indol-3-yl-methylene)-2-thioxo-imidazolidin-4-one (LPSF/NN-56) and 3-(4-Bromo-benzyl)-5-(1H-indol-3-yl-methylene)-2thioxo-imidazolidin-4-one (LPSF/NN-52) were evaluated using air pouch and carrageenan-induced peritonitis models as well as an acetic acid-induced vascular permeability model followed by IL-1β and TNF-α quantification. To evaluate the antinociceptive activities of the compounds, acetic acid-induced nociception, formalin and hot plate tests were also performed. The anti-inflammatory activities of the compounds were evidenced by a reduction in both leukocyte migration and the release of TNF-α and IL-1β in air pouch and peritonitis models. Upon acetic acid-induced nociception, a decrease in the level of abdominal writhing in the groups treated with LPSF/NN-52 (52.1%) or LPSF/NN-56 (63.1%) was observed. However, in the hot plate test, none of the derivatives tested exhibited an inhibition of nociception. These results indicate that the compounds tested exhibited promising anti-inflammatory and antinociceptive activities that likely involved the modulation of the immune system.

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Section: Discussionmentioning

confidence: 69%

Anti-inflammatory and antinociceptive activities of indole–imidazolidine derivatives

Guerra

Malta

Laranjeira

et al. 2011

International Immunopharmacology

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“…Likewise, hydrazones, thiazolidinone, and their bioisoster thiazole derivatives are known for their potential pharmaceutical applications and possess antimicrobial (23), antischistosomal (24), antifungal (25), antimalarial (26), herbicidal (27), antiviral (28), antidiabetic (29), and antioxidant (30) properties. Thiazole derivatives have been used to prepare various drugs that are important for antimicrobial (31), antibacterial (32,33), antifungal (32), antiinflammatory (34), and antitubercular (35) treatment, and some of the thiazole derivatives are used as antiprotozoals (36).…”

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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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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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“…The starting reagent was imidazolidine-2,4-dione (1) which was reacted with 2-chloro-6-fluorobenzyl chloride under basic conditions to obtain the intermediate 3-(2-chloro-6-fluorobenzyl) imidazolidine-2,4-dione as previously described (2) 20 . After that, the reaction of 3-(2-chloro-6-fluorobenzyl) imidazolidine-2,4-dione (2) with Lawesson’s reagent in anhydrous dioxane gave the compound 1-(2-chloro-6-fluorobenzyl)-5-thioxoimidazolidin-2-one (3) according to the protocol used by Gouveia et al 21 …”

Section: Methodsmentioning

confidence: 99%

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

Rocha

Lima

Silva

et al. 2017

Rev. Inst. Med. trop. S. Paulo

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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.

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Interaction of Morphine With a New α2-Adrenoceptor Agonist in Mice

Cited by 31 publications

References 45 publications

Anti-inflammatory and antinociceptive activities of indole–imidazolidine derivatives

Anti-inflammatory and antinociceptive activities of indole–imidazolidine derivatives

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

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

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