Characterization and analysis of the bioactivity of the Piper rivinoides Kunth essential oil and its components myristicin and elemicin, against opportunistic fungal pathogens.

Candidiasis is an infectious disease caused by some fungi of the genus Candida. In Brazil, the incidence rate is higher than in European countries and the United States, and health problems occur mainly due to the virulence factors of the fungi, which have made treatment with commercial drugs difficult. Considering the context, plants rich in phenolic compounds, such as those of the genus Piper, have been studied due to their antimicrobial properties.

(Baker) H. Rob. (Asteraceae), an Ordinary Bush or an Anti-Inflammatory and Immunomodulator Aromatic Species?

Oral traditional knowledge disseminates the use of young leaves of (Asteraceae) as poultice in feverish cases among family farmers in Santa Catarina, Brazil, but there is a lack of phytochemistry and pharmacological studies on this species, especially those related to volatile organic compounds. In the present study, the dry leaves of were subjected to hydrodistillation for the extraction of essential oil. Sample characterization was conducted using GC-FID and GC-MS.

In vitro and in silico effect of meldrum's acid-derived compounds on Staphylococcus aureus strains as NorA efflux pump inhibitors.

The misuse of antibiotics has led to an alarming increase in bacterial strains resistant to these drugs. Efflux pumps, which expel antibiotics from bacterial cells, have emerged as one of the key mechanisms of bacterial resistance. In the quest to combat and mitigate bacterial resistance, researchers have turned their attention to efflux pump inhibitors as a potential solution.

Meldrum's acid derivates are MepA efflux pump inhibitors: In vitro and in silico essays.

Efflux pumps are proteins capable of expelling antibiotics from bacterial cells, have emerged as a major mechanism of bacterial resistance. In the ongoing pursuit to overcome and reduce bacterial resistance, novel substances are being explored as potential efflux pump inhibitors. Meldrum's acid, a synthetic molecule widely studied for its role in synthesizing bioactive compounds, holds promise in this regard.

Efflux Pump (QacA, QacB, and QacC) and β-Lactamase Inhibitors? An Evaluation of 1,8-Naphthyridines against Strains.

The bacterial species presents a variety of resistance mechanisms, among which the expression of β-lactamases and efflux pumps stand out for providing a significant degree of resistance to clinically relevant antibiotics. The 1,8-naphthyridines are nitrogen heterocycles with a broad spectrum of biological activities and, as such, are promising research targets. However, the potential roles of these compounds on bacterial resistance management remain to be better investigated.

NorA, Tet(K), MepA, and MsrA Efflux Pumps in , their Inhibitors and 1,8-Naphthyridine Sulfonamides.

Antibiotic resistance can be characterized, in biochemical terms, as an antibiotic's inability to reach its bacterial target at a concentration that was previously effective. Microbial resistance to different agents can be intrinsic or acquired. Intrinsic resistance occurs due to inherent functional or structural characteristics of the bacteria, such as antibiotic-inactivating enzymes, nonspecific efflux pumps, and permeability barriers.

Chemical Profile and Biological Activities of Essential Oil from for Development and Improvement of Mouthwash.

Studies show that more consumers are using natural health products in the modern world. We have noticed a growing demand in markets and the professional community for mouthwashes that contain natural compounds. The objective of this study was to assess the chemical characterization and microbiological potential of the essential oil (EOPa) to provide data to enable the development of a low-cost mouthwash.

Enhancement of Antibiotic Activity by 1,8-Naphthyridine Derivatives against Multi-Resistant Bacterial Strains.

The search for new antibacterial agents has become urgent due to the exponential growth of bacterial resistance to antibiotics. Nitrogen-containing heterocycles such as 1,8-naphthyridine derivatives have been shown to have excellent antimicrobial properties. Therefore, the purpose of this study was to evaluate the antibacterial and antibiotic-modulating activities of 1,8-naphthyridine derivatives against multi-resistant bacterial strains.

Chemical synthesis, molecular docking and MepA efflux pump inhibitory effect by 1,8-naphthyridines sulfonamides.

This study aimed to evaluate the antibacterial activity and to verify, in silico and in vitro, the inhibition of efflux mechanisms using a series of synthesized 1,8-naphthyridines sulfonamides against Staphylococcus aureus strains carrying MepA efflux pumps. The chemical synthesis occurred through the thermolysis of the Meldrum's acid adduct. The sulfonamide derivatives were obtained by the sulfonylation of 2-amino-5‑chloro-1,8-naphthyridine with commercial benzenesulfonyl chloride.

Potentiation of Antibiotic Activity by a Meldrum's Acid Arylamino Methylene Derivative against Multidrug-Resistant Bacterial Strains.

This study aimed to evaluate the intrinsic antibacterial activity and antibiotic-enhancing effect of an arylamino methylene derivative (MAD) in association with fluoroquinolones. The antibacterial activity against multiresistant , and was analyzed by determining the minimum inhibitory concentration (MIC) using the broth micro dilution method. A reduction in the MIC of the fluoroquinolones against strains treated simultaneously with the MAD was interpreted as an enhanced antibiotic activity.

The 1,8-naphthyridines sulfonamides are NorA efflux pump inhibitors.

Objective: Efflux pumps are transmembrane proteins associated with bacterial resistance mechanisms. Bacteria use these proteins to actively transport antibiotics to the extracellular medium, preventing the pharmacological action of these drugs. This study aimed to evaluate in vitro the antibacterial activity of 1,8-naphthyridines sulfonamides, as well as their ability to inhibit efflux systems of Staphylococcus aureus strains expressing different levels of the NorA efflux pump.

Essential oils from leaves of (Spreng.) H. Rob.: chemical profile and antimollicute potential.

Aiming to valorise the Atlantic Rainforest biodiversity in Santa Catarina, the chemical characterisation of the essential oils (EOs) from leaves of (Spreng.) H. Rob.

Do 1,8-naphthyridine sulfonamides possess an inhibitory action against Tet(K) and MsrA efflux pumps in multiresistant Staphylococcus aureus strains?

Naphthyridines represent a class of heterocyclic compounds formed by two condensed aromatic rings. This study aimed to evaluate the antibacterial activity and in vitro inhibition of efflux resistance mechanisms of a series of 1,8-naphthyridine sulfonamides against strains carrying Tet(K) and MsrA efflux pumps. The efflux pump inhibitory capacity was evaluated by analyzing synergistic effects between 1,8-naphthyridine sulfonamides and standard antibiotics, as well as ethidium bromide.

GC/MS analysis and antimicrobial activity of the Piper mikanianum (Kunth) Steud. essential oil.

The Piper mikanianum species were investigated by the antimicrobial potential and chemical composition. Chemical analysis was performed by gas chromatography coupled to mass spectrometry (GC/MS). The Minimum Inhibitory Concentration (MIC) as well as the 50% Inhibitory Concentration against Candida strains were determined by microdilution.

Piper diospyrifolium Kunth.: Chemical analysis and antimicrobial (intrinsic and combined) activities.

The secular use of plants in popular medicine has emerged as a source for the discovery of new compounds capable of curing infections. Among microbial resistance to commercial drugs, species such as Piper diospyrifolium Kunth, which are used in popular therapy, are targets for pharmacological studies. With this in mind, antimicrobial experiments with the essential oil from the P.

Synthesis of 1,8-naphthyridines and their application in the development of anionic fluorogenic chemosensors.

Two 1,8-naphthyridines were synthesized and found to be fluorescent in solution. These compounds were studied in the presence of Cu(+) and Cu(2+) ions and it was verified that the metal causes the quenching of their fluorescence emission, due to the formation of complexes between the naphthyridine and the metal. A displacement assay was carried out in a DMSO-water mixture with the addition of various anions to the solutions of the complexes, and it was observed that these systems have a high capacity to selectively detect cyanide.

Synthesis and in vitro evaluation of leishmanicidal and trypanocidal activities of N-quinolin-8-yl-arylsulfonamides.

In the present paper 12 N-quinolin-8-yl-arylsulfonamides synthesized by coupling 8-aminoquinolines with various arylsulfonylchlorides were assayed in vitro against Leishmania amazonensis, Leishmania chagasi and Trypanosoma cruzi strains. This series of new compounds were found to be selective for Leishmania spp. promastigote and amastigote forms.

4,5,6,8,9-Pentachloropyrimido[1,2-a][1,8]naphthyridin-10-one.

The title compound, C11H2Cl5N3O, crystallizes in the monoclinic system with two molecules in the asymmetric unit. The molecules are chemically identical but have different structural parameters. In the three-dimensional packing, the molecules are arranged in dimers that are connected by slipped pi-pi stacking, and these dimers are connected to one another through several C-H.