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4-Phenyl-1,3-thiazole-2-amines as scaffolds for new antileishmanial agents J. Venom. Anim. Toxins incl. Trop. Dis.
Rodrigues,Carina Agostinho; Santos,Paloma Freire dos; Costa,Marcela Oliveira Legramanti da; Pavani,Thais Fernanda Amorim; Xander,Patrícia; Geraldo,Mariana Marques; Mengarda,Ana; Moraes,Josué de; Rando,Daniela Gonçales Galasse.
Abstract Background: There is still a need for new alternatives in pharmacological therapy for neglected diseases, as the drugs available show high toxicity and parenteral administration. That is the case for the treatment of leishmaniasis, particularly to the cutaneous clinical form of the disease. In this study, we present the synthesis and biological screening of eight 4-phenyl-1,3-thiazol-2-amines assayed against Leishmania amazonensis. Herein we propose that these compounds are good starting points for the search of new antileishmanial drugs by demonstrating some of the structural aspects which could interfere with the observed activity, as well as suggesting potential macromolecular targets. Methods: The compounds were easily synthesized by the...
Tipo: Info:eu-repo/semantics/article Palavras-chave: 2-aminothiazoles; Antikinetoplastids; Antileishmanial; Cutaneous; Target fishing.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992018000100317
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Antileishmanial activity and immunomodulatory effect of secosubamolide, a butanolide isolated from Nectandra oppositifolia (Lauraceae) J. Venom. Anim. Toxins incl. Trop. Dis.
Costa-Silva,Thais A. da; Conserva,Geanne A. Alves; Galisteo Jr,Andrés J.; Tempone,Andre G.; Lago,João Henrique G..
Abstract Background: Visceral leishmaniasis is a complex neglected tropical disease caused by Leishmania donovani complex. Its current treatment reveals strong limitations, especially high toxicity. In this context, natural products are important sources of new drug alternatives for VL therapy. Therefore, the antileishmanial and immunomodulatory activity of compounds isolated from Nectandra oppositifolia (Lauraceae) was investigated herein. Methods: The n-hexane extract from twigs of N. oppositifolia were subjected to HPLC/HRESIMS and bioactivity-guided fractionation to afford compounds 1 and 2 which were evaluated in vitro against Leishmania (L.) infantum chagasi and NCTC cells. Results: The n-hexane extract displayed activity against L. (L.) infantum...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Leishmania (L.) infantum chagasi; Antileishmanial; Nectandra oppositifolia; Secosubamolide; Immunomodulatory.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992019000100317
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Essential oil of Mitracarpus frigidus as a potent source of bioactive compounds Anais da ABC (AABC)
Fabri,Rodrigo L.; Coimbra,Elaine S.; Almeida,Ana C.; Siqueira,Ezequias P.; Alves,Tânia M.A.; Zani,Carlos L.; Scio,Elita.
In our previous work (Fabri et al. 2009), we showed that different extracts of Mitracarpus frigidus had significant antibacterial, antifungal and leishmanicidal activities. In order to increase our knowledge about this species, this work assesses the chemical composition and the in vitro biological activity of its essential oil. Thus, the essential oil obtained by hydrodistillation of the aerial parts of M. frigidus was analyzed by GC/MS. Among several compounds detected, 11 were identified, being linalool and eugenol acetate the major components. The essential oil exhibited a moderate antibacterial effect against Staphyloccocus aureus, Bacillus cereus, Pseudomonas aeruginosa and Enterobacter cloacae (MIC 250 µg/mL). On the other hand, it showed a strong...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Mitracarpus frigidus; Essential oil; Antimicrobial; Antileishmanial; Cytotoxicity.
Ano: 2012 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652012000400021
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In Vitro Assessment of Antileishmanial Activity of Natamycin and Nystatin BABT
Sidana,Arushdeep; Negi,Ajeet Kumar; Farooq,Umar.
ABSTRACT The present study was aimed to evaluate the in vitro antileishmanial activity of four different concentrations of natamycin and nystatin by using MTT 3-(4.5-dimethylthiazol-2-yl)-2.5-diphenyl tetrazolium bromide reduction assay. In vitro antileishmanial activity revealed that the IC50 of natamycin (80.49 μg/ml) and nystatin (105.7 μg/ml) was less than that of sodium stibogluconate (127.9 μg/ml), and more than amphotericin B (18.91 μg/ml).
Tipo: Info:eu-repo/semantics/article Palavras-chave: Leishmaniasis; Leishmania donovani; Antileishmanial; Natamycin; Nystatin.
Ano: 2017 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-89132017000100301
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