Effect of thiadiazine derivatives on intracellular amastigotes of Leishmania amazonensis

Fidalgo, Lianet Monzote; Álvarez, Alina; Géigel, Lisset Fonseca; Perez-Pineiro, Rolando; Navarro, Margarita Suárez; Cabrera, Hortensia Rodríguez

doi:10.1590/s0074-02762004000300016

Cited by 18 publications

(3 citation statements)

References 7 publications

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“…They are safe, cheaper and partly available in endemic countries. [22][23][24][25] Therefore, the research on the antileishmanial effects of medicinal plants is urgently essential. In this study, the antileishmanial effects of the ethanolic extracts of Ixora brachiata root on L. major and L. infantum promastigotes were evaluated by MTT assay.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

Eskandari

Khademvatan

Nejad³

et al. 2019

Int J Enteric Pathog

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Background: Leishmaniasis is a major global health problem which affects millions of people, especially in the developing countries. The incidence of leishmaniasis has increased and there is no vaccination for Leishmania infections and standard drugs for treatment of the disease have many side effects; therefore, it is necessary to find new effective alternatives. Objectives: The purpose of this study was to evaluate the in vitro antileishmanial activity of Ixora brachiata root extract against Leishmania major and Leishmania infantum promastigotes. Materials and Methods: Different doses of the selected plant extract was tested against L. major and L. infantum promastigotes using colorimetric MTT [3-(4, 5-methylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide] assay. Glucantime was used as the positive control. Results: Anti-parasitic activity was revealed for I. brachiata root on L. major and L. infantum with 50% inhibitory concentration (IC50) values of 0.91 and 2.63 µg/mL, respectively compared to the standard drugs, glucantime, which had an IC50 value of 40.2 µg/mL for L. major and 18.5 µg/ mL for L. infantum after 72 hours. Conclusion: The results of this study created a new background on the development of drug against leishmania parasite.

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Section: Discussionmentioning

confidence: 99%

Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

Eskandari

Khademvatan

Nejad³

et al. 2019

Int J Enteric Pathog

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“…Compounds were purified on Merck ® 60 silica gel (particle size 0.040-0.063 nm) or using Armen ® spot flash chromatography (normal phase column: Interchim 30 SHIP 25 g; reverse phase column: AIT 50 g C18). 1 H and 13 C NMR spectra were recorded on Bruker ® Avance III Spectrometer operating at 600 and 150 MHz, respectively. The chemical shifts were reported in δ units, and coupling constants (J) were measured in hertz.…”

Section: Acquisition Of the Isolated Substancesmentioning

confidence: 99%

“…Thiadiazines are heterocyclic compounds that contain two nitrogen atoms and one sulfur atom in their structure [11]. These synthetic molecules have several relevant pharmacological activities, such as antifungal [12], antibacterial [10], and antiparasitic [13]. However, the modifying activity of antibiotics against MDR strains by substances from the thiadiazine group remains unknown.…”

Section: Introductionmentioning

confidence: 99%

Potentiating‐antibiotic activity and absorption, distribution, metabolism, excretion and toxicity properties (ADMET) analysis of synthetic thiadiazines against multi‐drug resistant (MDR) strains

de Araújo,

Freitas,

Araújo

et al. 2023

Fundamemntal Clinical Pharma

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BackgroundThiadiazines are heterocyclic compounds that contain two nitrogen atoms and one sulfur atom in their structure. These synthetic molecules have several relevant pharmacological activities, such as antifungal, antibacterial, and antiparasitic.ObjectivesThe present study aimed to evaluate the possible in vitro and in silico interactions of compounds derived from thiadiazines.MethodsThe compounds were initially synthesized, purified, and confirmed through HPLC methodology. Multi‐drug resistant bacterial strains of Staphylococcus aureus 10 and Pseudomonas aeruginosa 24 were used to evaluate the direct and modifying antibiotic activity of thiadiazine derivatives. ADMET assays (absorption, distribution, metabolism, excretion, and toxicity) were conducted, which evaluated the influence of the compounds against thousands of macromolecules considered as bioactive targets.ResultsThere were modifications in the chemical synthesis in carbon 4 or 3 in one of the aromatic rings of the structure where different ions were added, ensuring a variability of products. It was possible to observe results that indicate the possibility of these compounds acting through the cyclooxygenase 2 mechanism, which, in addition to being involved in inflammatory responses, also acts by helping sodium reabsorption. The amine group present in thiadiazine analogs confers hydrophilic characteristics to the substances, but this primary characteristic has been altered due to alterations and insertions of other ligands. The characteristics of the analogs generally allow easy intestinal absorption, reduce possible hepatic toxic effects, and enable possible neurological and anti‐inflammatory action. The antibacterial activity tests showed a slight direct action, mainly of the IJ23 analog. Some compounds were able to modify the action of the antibiotics gentamicin and norfloxacin against multi‐drug resistant strains, indicating a possible synergistic action.ConclusionsAmong all the results obtained in the study, the relevance of thiadiazine analogs as possible coadjuvant drugs in the antibacterial, anti‐inflammatory, and neurological action with low toxicity is clear. Need for further studies to verify these effects in living organisms is not ruled out.

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¹H and ¹³C NMR spectral assignment of alkyl and polyamine‐linked bis(2‐thioxo‐[1,3,5]‐thiadiazinan‐3‐yl) carboxylic acids

Molero

Coro

Pérez

et al. 2006

Magnetic Reson in Chemistry

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Effect of thiadiazine derivatives on intracellular amastigotes of Leishmania amazonensis

Cited by 18 publications

References 7 publications

Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

Potentiating‐antibiotic activity and absorption, distribution, metabolism, excretion and toxicity properties (ADMET) analysis of synthetic thiadiazines against multi‐drug resistant (MDR) strains

¹H and ¹³C NMR spectral assignment of alkyl and polyamine‐linked bis(2‐thioxo‐[1,3,5]‐thiadiazinan‐3‐yl) carboxylic acids

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Effect of thiadiazine derivatives on intracellular amastigotes of Leishmania amazonensis

Cited by 18 publications

References 7 publications

Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

Evaluation of the Antileishmanial Properties of Ixora brachiata Roxb on Leishmania major and Leishmania infantum by Colorimetric MTT Assay

Potentiating‐antibiotic activity and absorption, distribution, metabolism, excretion and toxicity properties (ADMET) analysis of synthetic thiadiazines against multi‐drug resistant (MDR) strains

1H and 13C NMR spectral assignment of alkyl and polyamine‐linked bis(2‐thioxo‐[1,3,5]‐thiadiazinan‐3‐yl) carboxylic acids

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¹H and ¹³C NMR spectral assignment of alkyl and polyamine‐linked bis(2‐thioxo‐[1,3,5]‐thiadiazinan‐3‐yl) carboxylic acids