The design, synthesis, docking studies and evaluation of the antifungal and cytotoxic properties of eugenol (EUG) containing 1,2,3-triazole derivatives are reported. Most of the derivatives have not been reported. The EUG derivatives were synthesized, molecular docked and tested for their antifungal activity.
View Article and Find Full Text PDFRev Soc Bras Med Trop
July 2024
Background: The current treatments for Chagas disease (CD) include benznidazole and nifurtimox, which have limited efficacy and cause numerous side effects. Triazoles are candidates for new CD treatments due to their ability to eliminate T. cruzi parasites by inhibiting ergosterol synthesis, thereby damaging the cell membranes of the parasite.
View Article and Find Full Text PDFFuture Med Chem
August 2024
This study aimed to enhance the aqueous dissolution of SRPK inhibitor -(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)isonicotinamide (SRPIN340). A complex with -sulfonic calix[6]arene (Host) and SRPIN340 (Guest) was prepared, studied via H nuclear magnetic resonance (NMR) and theoretical calculations and biologically evaluated on cancer cell lines. The 1:1 host (H)/guest (G) complex significantly enhanced the aqueous dissolution of SRPIN340, achieving 64.
View Article and Find Full Text PDFThis study explores the stabilization by niobic acid, of Pt, Ni, Pd, and Au nanoparticles (NPs) for the efficient microheterogeneous catalysis of NaBH hydrolysis for hydrogen production. Niobic acid is the most widely studied NbO polymorph, and it is employed here for the first time for this key reaction relevant to green energy. Structural insights from XRD, Raman, and FTIR spectroscopies, combined with hydrogen production data, reveal the role of niobic acid's Brønsted acidity in its catalytic activity.
View Article and Find Full Text PDFMethicillin-resistant Staphylococcus aureus (MRSA) is widely recognized as a causative agent for various infections acquired in healthcare settings as well as in the community. Given the limited availability of effective antimicrobial agents to combat MRSA infections, there is an increasing need to explore alternative therapeutic strategies. This study aimed to assess the antimicrobial, anti-adhesive, anti-biofilm properties, and toxicity of 175 newly synthesized compounds, belonging to seven different classes, against MRSA.
View Article and Find Full Text PDFTreatment against leishmaniasis presents problems, mainly due to the toxicity of the drugs, high cost, and the emergence of resistant strains. A previous study showed that two vanillin-derived synthetic molecules, 3s [4-(2-hydroxy-3-(4-octyl-1H-1,2,3-triazol-1-yl)propoxy)-3-methoxybenzaldehyde] and 3t [4-(3-(4-decyl-1H-1,2,3-triazol-1-yl)-2-hydroxypropoxy)-3-methoxybenzaldehyde], presented antileishmanial activity against Leishmania infantum, L. amazonensis, and L.
View Article and Find Full Text PDFTreatment against visceral leishmaniasis (VL) presents problems, mainly related to drug toxicity, high cost and/or by emergence of resistant strains. In the present study, two vanillin synthetic derivatives, 3 s [4-(2-hydroxy-3-(4-octyl-1H-1,2,3-triazol-1-yl)propoxy)-3-methoxybenzaldehyde] and 3 t [4-(3-(4-decyl-1H-1,2,3-triazol-1-yl)-2-hydroxypropoxy)-3-methoxybenzaldehyde], were evaluated as therapeutic candidates in a murine model against Leishmania infantum infection. Molecules were used pure (3 s and 3 t) or incorporated into Poloxamer 407-based micelles (3 s/M and 3 t/M) in the infected animals, which also received amphotericin B (AmpB) or Ambisome® as control.
View Article and Find Full Text PDFFuture Med Chem
January 2024
The assessment of the antileishmanial potential of 22 vanillin-containing 1,2,3-triazole derivatives against is reported. Initial screening was performed against the parasite promastigote form. The most active compound, , targeted parasites within amastigotes (IC = 4.
View Article and Find Full Text PDFChagas disease is a life-threatening illness caused by . The involvement of serine-/arginine-rich protein kinase in the life cycle is significant. To synthesize, characterize and evaluate the trypanocidal activity of diamides inspired by kinase inhibitor, SRPIN340.
View Article and Find Full Text PDFPharmaceuticals (Basel)
August 2023
Leishmaniasis is a group of infectious diseases caused by protozoan parasites that belong to the genus . Currently, there is no human vaccine, and the available treatments are associated with toxicity, high cost, and the emergence of resistant strains. These factors highlight the need to identify new antileishmanial candidates.
View Article and Find Full Text PDFMolecules
August 2023
The present investigation aimed to develop inclusion complexes (ICs) from (GAU) essential oil (EO) and its major compound -caryophyllene (-CAR), and to evaluate their herbicidal (against and ) and cytogenotoxic (on ) activities. The ICs were obtained using 2-hydroxypropyl--cyclodextrin (HPCD) and they were prepared to avoid or reduce the volatility and degradation of GAU EO and -CAR. The ICs obtained showed a complexation efficiency of 91.
View Article and Find Full Text PDFLung cancer is the leading cause of cancer mortality worldwide, and malignant melanomas are highly lethal owing to their elevated metastatic potential. Despite improvements in therapeutic approaches, cancer treatments are not completely effective. Thus, new drug candidates are continuously sought.
View Article and Find Full Text PDFDiscovery of novel SARS-CoV-2 main protease (M) inhibitors using a structure-based drug discovery strategy. Virtual screening employing covalent and noncovalent docking was performed to discover M inhibitors, which were subsequently evaluated in biochemical and cellular assays. 91 virtual hits were selected for biochemical assays, and four were confirmed as reversible inhibitors of SARS CoV-2 M with IC values of 0.
View Article and Find Full Text PDFExp Parasitol
August 2023
The treatment against leishmaniasis presents problems, mainly due to their toxicity of the drugs, high cost and/or by the emergence of parasite resistant strains. In this context, new therapeutics should be searched. In this study, two novel synthetic derivatives from vanillin: [4-(2-hydroxy-3-(4-octyl-1H-1,2,3-triazol-1-yl)propoxy)-3-methoxybenzaldehyde] or 3s and [4-(3-(4-decyl-1H-1,2,3-triazol-1-yl)-2-hydroxypropoxy)-3-methoxybenzaldehyde] or 3t, were evaluated regarding their antileishmanial activity against distinct parasite species able to cause cutaneous and visceral leishmaniasis.
View Article and Find Full Text PDFIn agriculture, the control of fungal infections is essential to improve crop quality and productivity. This study describes the preparation and fungicidal activity evaluation of 12 glycerol derivatives bearing 1,2,3-triazole fragments. The derivatives were prepared from glycerol in four steps.
View Article and Find Full Text PDFThe Zika virus (ZIKV) is an arbovirus and belongs to the Flaviviridae family and Flavivirus genus, with dissemination in the Americas. In Brazil, the predominant strain is the Asian, promoting outbreaks that started in 2015 and are directly related to microcephaly in newborns and Guillain-Barré syndrome in adults. Recently, researchers identified a new African strain circulating in Brazil at the mid-end of 2018 and the beginning of 2019, with the potential to originate a new epidemic.
View Article and Find Full Text PDFVanillin is the main component of natural vanilla extract and is responsible for its flavoring properties. Besides its well-known applications as an additive in food and cosmetics, it has also been reported that vanillin can inhibit fungi of clinical interest, such as Candida spp., Cryptococcus spp.
View Article and Find Full Text PDFActa Trop
February 2023
Leishmaniasis is a parasitic disease found in tropical and subtropical regions around the world, caused by parasites of the genus Leishmania. The disease is a public health concern and presents clinical manifestations that can cause death, disability, and mutilation. The parasite has promastigote (vector) and amastigote (vertebrate host) forms and kinase enzymes are involved in this differentiation process.
View Article and Find Full Text PDFFew extracts of plant species from the Brazilian flora have been validated from a pharmacological and clinical point of view, and it is important to determine whether their traditional use is proven by pharmacological effects. is one of those plants, which belongs to the Fabaceae family that is widely used in traditional medicine and is very rich in tannins. Due to the lack of effective drugs to treat severe cases of Covid-19, the main protease of SARS-CoV-2 (M) becomes an attractive target in the research for new antivirals since this enzyme is crucial for virus replication and does not have homologs in humans.
View Article and Find Full Text PDFBiomass valorization is essential, particularly in emerging countries. Here, hydrochar from arabica coffee straw was functionalized with a triazole group (HD-TRz) for use as a support of palladium nanoparticles (PdNPs-HD-TRz) applied in the Ullmann coupling reaction for the first time. It provided remarkably excellent selectivities, conversions at a temperature as low as 45 °C and catalyst recyclability, surpassing previous literature performances.
View Article and Find Full Text PDFNat Prod Res
June 2023
Inclusion complexes (ICs) of 2-hydroxypropyl-β-cyclodextrin with the essential oil (EO) from Seculo XXI cultivar of were prepared using kneading (KN) and freeze-drying (FD) methods. The resulting ICs clusters have a nanometric size, with a diameter of approximately 80 and 40 nm for KN and FD, respectively. Complexation efficiency was 80.
View Article and Find Full Text PDFLife Sci
October 2022
The serine/arginine-rich protein kinases (SRPK) specifically phosphorylate their substrates at RS-rich dipeptides, which are abundantly found in SR splicing factors. SRPK are classically known for their ability to affect the splicing and expression of gene isoforms commonly implicated in cancer and diseases associated with infectious processes. Non-splicing functions have also been attributed to SRPK, which highlight their functional plasticity and relevance as therapeutic targets for pharmacological intervention.
View Article and Find Full Text PDFBiochem Pharmacol
September 2022
Cancers have a strong relationship with immune cells in their microenvironment, which significantly influences tumor proliferation and progression. Thus, pharmacological strategies that stimulate the immune system to combat tumor cells are promising for better therapeutic efficacy. Deregulated expression of the splicing regulatory serine arginine protein kinases (mostly SRPK1 and SRPK2) has been found in different cancer types, leading to the expression of isoforms related to tumor growth and metastasis.
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