Antiviral activity of indole derivatives

Giampieri, Michele; Balbi, Alessandro; Mazzei, Mauro; Colla, Paolo La; Ibba, Cristina; Loddo, Roberta

doi:10.1016/j.antiviral.2009.05.001

Cited by 64 publications

(29 citation statements)

References 5 publications

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“…(ANOVA), when control groups were compared to test groups **p<0.05 (ANOVA) when compared to Glucantime (Glu) and Azythromicine (Azy) this study (Peyron et al 2005;Storch et al 2007;Giampieri et al 2009). The citotoxicity assays are important as to detect if the drug has a potential of being used against the intramacrophagic forms of the parasite.…”

Section: Discussionmentioning

confidence: 99%

Morphological alterations and growth inhibition of Leishmania (L.)amazonensis promastigotes exposed to zidovudine (AZT)

Araújo

Batista

et al. 2010

Parasitol Res

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Leishmania parasites cause a worldwide public health disease and its treatment is still based on pentavalent antimonials which present financial and toxicologic limitations. Some nucleosidic derivatives have demonstrated anti-leishmanial properties and this study aims to evaluate the in vitro morphologic alterations and growth inhibition of Leishmania (L.) amazonensis promastigotes exposed to zidovudine at several concentrations. The citotoxicity of zidovudine (AZT) to macrophages was determined by an MTT assay. After which the promastigotes were exposed to concentrations of AZT, ranging from 1 to 50 μM. The evaluation of survival and morphometry alterations were performed in two distinct phases of in vitro growth, on the third and sixth days, representing the logarithmic and stationary phases, respectively. Slides with the promastigotes were photographed and analyzed using Image J. A significant reduction of parasite number in the logarithmic phase of in vitro growth was observed when the parasites were submitted to 20, 30, 40, and 50 μM of AZT. Morphometric alterations were observed such as an increase in width of the body, cytoplasmic granulations and vacuolizations. These data indicate the toxicity of AZT which prevents the parasite's multiplication, indicating a promising use of AZT as an anti-leishmania drug.

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Section: Discussionmentioning

confidence: 99%

Morphological alterations and growth inhibition of Leishmania (L.)amazonensis promastigotes exposed to zidovudine (AZT)

Araújo

Batista

et al. 2010

Parasitol Res

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“…On the other hand, indole derivatives have been a topic of substantial research interest in contemporary heterocyclic and medicinal chemistry due to their great significance in the view of their (i) occurrence in nature as a prominent sub-structure of a large number of alkaloids (Tanaka et al, 2006;Frederich et al, 2008) and (ii) wide-ranging biological activities which includes antimicrobial (Al-Qawasmeh et al, 2010;Tiwari et al, 2006;Harnden et al, 1978), antitubercular (Karthikeyan et al, 2009;Guzel et al, 2008), ghrelin receptor (Demange et al, 2007), anticancer (Singh et al, 2009;Shi et al, 2007), antioxidant (Lakshmi et al, 2010), antiviral (Giampieri et al, 2009;Fonseca et al, 2004), and antimalarial (Kgokong et al, 2005;Agarwal et al, 2005). Literature survey manifests that the number of 4H-chromene derivatives have been synthesized using various aldehydes Patel, 2009a, 2011b;Mungra et al, 2011b) but there is not a single report where 2-phenyl-1H-indole-3-carbaldehyde is used.…”

Section: Introductionmentioning

confidence: 99%

Microwave-assisted synthesis of 3′-indolyl substituted 4H-chromenes catalyzed by DMAP and their antimicrobial activity

Kathrotiya

Patel

2011

Med Chem Res

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A new series of indole-based chromene derivatives 4a-4p has been synthesized by one pot cyclocondensation reaction of 2-phenyl-1H-indole-3-carbaldehyde 1a-1h; malononitrile 2; and 1,3-cyclohexanedione/dimedone 3a/b under microwave irradiation catalyzed by an organocatalyst 4-(N,N-dimethylamino) pyridine. Easy experimental procedure, high yield, selectivity, and shorter reaction time are the imperative features of this method. All the compounds were screened against a representative panel of bacteria and fungi. Some of the compounds are found to be equipotent or more potent than that of standard drugs as evident from SAR study.

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“…This has allowed researchers to understand the structureactivity relationship (SAR) in addition to developing novel, more effective lead compounds for inhibition of BVDV replication. Discovery of small molecule inhibitors of BVDV RdRp as a potential therapeutic target has been reported in the literature with various scaffolds, such as imidazopyridines, [7][8][9][10][11] benzimidazole derivatives, 12,13 arylazoenamines, 14,15 indole derivatives, 16 γ-carboline derivatives, 17 thiosemicabarzone, 18 diphenylmethane, 19,20 and aromatic cationic molecules. 21,22 The majority of anti-BVDV inhibitors could also be taken as an accurate measurement of antiviral activity against HCV or other Pestiviruses (e.g., CSFV, BDV) and Flaviviruses (e.g., YFV, WNV, DENV) in the same family for the purpose of exploiting approved treatments.…”

Section: Introductionmentioning

confidence: 99%

Molecular Modeling of Small Molecules as BVDV RNA-Dependent RNA Polymerase Allosteric Inhibitors

Chai¹,

Lim²,

Chai³

et al. 2013

Bulletin of the Korean Chemical Society

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Bovine viral diarrhea virus (BVDV), a major pathogen of cattle, is a well-characterized pestivirus which has been used as a good model virus for HCV. The RNA-dependent RNA polymerase (RdRp) plays a key role in the RNA replication process, thus it has been targeted for antivirus drugs. We employed two-dimensional quantitative structure-activity relationship (2D-QSAR) and molecular field analysis (MFA) to identify the molecular substructure requirements, and the particular characteristics resulted in increased inhibitory activity for the known series of compounds to act as effective BVDV inhibitors. The 2D-QSAR study provided the rationale concept for changes in the structure to have more potent analogs focused on the class of arylazoenamines, benzimidazoles, and acridine derivatives with an optimal subset of descriptors, which have significantly contributed to overall anti-BVDV activity. MFA represented the molecular patterns responsible for the actions of antiviral compound at their receptors. We conclude that the polarity and the polarizability of a molecule play a main role in the inhibitory activity of BVDV inhibitors in the QSAR modeling.

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Antiviral activity of indole derivatives

Cited by 64 publications

References 5 publications

Morphological alterations and growth inhibition of Leishmania (L.)amazonensis promastigotes exposed to zidovudine (AZT)

Morphological alterations and growth inhibition of Leishmania (L.)amazonensis promastigotes exposed to zidovudine (AZT)

Microwave-assisted synthesis of 3′-indolyl substituted 4H-chromenes catalyzed by DMAP and their antimicrobial activity

Molecular Modeling of Small Molecules as BVDV RNA-Dependent RNA Polymerase Allosteric Inhibitors

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