Synthesis of 1,3,4-oxadiazoles with 4-methoxynaphthalene ring: discovering new compounds with antimicrobial activity.

Paracoccidioidomycosis (PCM) is a systemic infection caused by spp. (). PCM can be associated or clinically confused with tuberculosis (TB), another pulmonary infection, caused by ().

Isoniazid-N-acylhydrazones as promising compounds for the anti-tuberculosis treatment.

Tuberculosis (TB), a disease caused by Mycobacterium tuberculosis complex, still presents significant numbers of incidence and mortality, in addition to several cases of drug resistance. Resistance, especially to isoniazid, which is one of the main drugs used in the treatment, has increased. In this context, N-acylhydrazones derived from isoniazid have shown important anti-Mycobacterium tuberculosis activity.

Essential oil of is active against mycobacteria.

There is critical need for new therapeutic options for treatment of diseases caused by mycobacteria. essential oils (EOs) and crude extracts (CEs) were tested for their anti- and anti-nontuberculous mycobacteria activity. Minimum inhibitory concentration (MIC) of EOs ranged from 15.

Polymyxin B Activity Rescue by (-)-Camphene-Based Thiosemicarbazide Against Carbapenem-Resistant .

Due to the significant shortage of therapeutic options for carbapenem-resistant (CRE) infections, new drugs or therapeutic combinations are urgently required. We show in this study that (-)-camphene-based thiosemicarbazide (TSC) may act synergistically with polymyxin B (PMB) against CRE, rescuing the activity of this antimicrobial. With the specific aim of a better molecular understanding of this effect caused by the presence of TSC, theoretical calculations were also performed in this study.

3,5-dinitrobenzoylhydrazone derivatives as a scaffold for antituberculosis drug development.

The development of drugs is essential to eradicate tuberculosis. Sixteen 3,5-dinitrobenzoylhydrazone () derivatives and their synthetic precursors 3,5-dinitrobenzoylhydrazide () and methyl ester () were screened for their anti- () potential. Twelve compounds had minimum inhibitory concentration (MIC) ranging from 0.

Phytoprostane and phenolic compounds from .

The chemical investigation of (Sch.Bip Baker) R.M.

Rescue of streptomycin activity by piperine in .

To evaluate the modulatory effect of piperine (PIP) on streptomycin (SM) activity in (). SM and PIP minimum inhibitory concentration (MIC) and combinatory activity were determined in HRv and in susceptible and resistant clinical isolates. Ethidium bromide accumulation assay and relative quantification of efflux pumps genes ( and ), after SM and SM+PIP combination exposure, were also performed.

and Evaluations of Anti- Activity of Benzohydrazones Compounds.

Tuberculosis is a disease caused by , with high mortality rates and an extended treatment that causes severe adverse effects, besides the emergence of resistant bacteria. Therefore, the search for new compounds with anti- activity has considerably increased in recent years. In this context, benzohydrazones are significant compounds that have antifungal and antibacterial action.

Antituberculosis Activities of Lapachol and β-Lapachone in Combination with Other Drugs in Acidic pH.

The treatment of multidrug-resistant tuberculosis (MDR-TB) is a challenge to be overcome. The increase of resistant isolates associated with serious side effects during therapy leads to the search for substances that have anti-TB activity, which make treatment less toxic, and also act in the macrophage acidic environment promoted by the infection. The aim of this study was to investigate lapachol and β-lapachone activities in combination with other drugs against at neutral and acidic pH and its cytotoxicity.

Synthesis and biological evaluation of 12 novel (-)-camphene-based 1,3,4-thiadiazoles against .

To evaluate the activity, cytotoxicity and efflux pumps inhibition of a series of 12 novels (-)-camphene-based 1,3,4-thiadiazoles (TDZs) against (). The minimum inhibitory concentration (MIC), cytotoxicity for three cell lines, ethidium bromide accumulation and checkerboard methods were carried out. Compounds (, , , , and ) showed significant anti- activity (MIC 3.

Determination of minimum bactericidal concentration, in single or combination drugs, against .

To evaluate an assay to detect minimum bactericidal concentration (MBC) in , using as single model rifampicin, isoniazid, levofloxacin (LVX) and linezolid (LNZ) and in combination. MBCs were carried out directly from resazurin microtiter assay plate and 3D checkerboard in HRv and five resistant clinical isolates. The proposed MBC assay showed similar values to those determined by MGIT™, used as control.

Minimum Bactericidal Concentration Techniques in : A Systematic Review.

Minimum bactericidal concentration (MBC) assay is an accepted parameter for evaluating new antimicrobial agents, and it is frequently used as a research tool to provide a prediction of bacterial eradication. To the best of our knowledge, there is no standardization among researchers regarding the technique used to detect a drug's MBC in . Thus, the aim of this systematic review is to discuss the available literature in determining a drug's MBC in , to find the most commonly used technique and standardize the process.

Hydrazone, benzohydrazones and isoniazid-acylhydrazones as potential antituberculosis agents.

To evaluate the potential of three benzohydrazones (-), four acylhydrazones derived from isoniazid (INH-acylhydrazones) (-) and one hydrazone () as antituberculosis agents. Inhibitory and bactericidal activities were determined for the reference () strain and clinical isolates. Cytotoxicity, drug combinations and ethidium bromide accumulation assays were also performed.

Novel 4-methoxynaphthalene--acylhydrazones as potential for paracoccidioidomycosis and tuberculosis co-infection.

 17 new 4-methoxynaphthalene--acylhydrazones were synthesized in order to evaluate their biological action against important pathogens.   susceptibility assays of compounds were performed against and . Compounds , and were the most potent against , two with minimum inhibitory concentrations of ≤1 μg ml and exhibited pharmacological synergy with amphotericin B.

Eugenol and derivatives activity against Mycobacterium tuberculosis, nontuberculous mycobacteria and other bacteria.

Aim: To evaluate (i) the in vitro activity of eugenol (EUG) and three derivatives against Mycobacterium tuberculosis (Mtb), nontuberculous mycobacteria (NTM) and other bacteria, (ii) the EUG and antituberculosis drugs combinatory effect and (iii) the EUG and its derivatives cytotoxicity.

Materials & Methods: Minimum inhibitory concentration of the compounds were determined by resazurin microtiter or broth microdilution assay and the drug interaction between EUG and antituberculosis drugs by resazurin drug combination microtiter. The cytotoxicity was carried out in macrophages, HeLa and VERO cells.