A5087157135- Tuberculosis Research and Epidemiology
- Synthesis and biological activity
- Mycobacterium research and diagnosis
- Phenothiazines and Benzothiazines Synthesis and Activities
- Bioactive Compounds and Antitumor Agents
- Cancer therapeutics and mechanisms
- Infectious Diseases and Mycology
- Antibiotic Resistance in Bacteria
- Synthesis and Biological Evaluation
- Sesquiterpenes and Asteraceae Studies
- Antifungal resistance and susceptibility
- Infectious Diseases and Tuberculosis
- Trypanosoma species research and implications
- Click Chemistry and Applications
- Plant-Derived Bioactive Compounds
- Essential Oils and Antimicrobial Activity
- Synthesis and Reactions of Organic Compounds
- Phytochemistry and Bioactivity Studies
- Fungal Infections and Studies
- Multicomponent Synthesis of Heterocycles
- Quinazolinone synthesis and applications
- Phytochemical compounds biological activities
- Sulfur-Based Synthesis Techniques
- Antimicrobial agents and applications
- Piperaceae Chemical and Biological Studies
Universidade Estadual de Maringá
2015-2025
Universidade Tecnológica Federal do Paraná
2020
Aim: To evaluate (i) the in vitro activity of eugenol (EUG) and three derivatives against Mycobacterium tuberculosis (Mtb), nontuberculous mycobacteria (NTM) other bacteria, (ii) EUG antituberculosis drugs combinatory effect (iii) its cytotoxicity. Materials & methods: Minimum inhibitory concentration compounds were determined by resazurin microtiter or broth microdilution assay drug interaction between combination microtiter. The cytotoxicity was carried out macrophages, HeLa VERO cells....
The search for new drugs to treat tuberculosis and nontuberculous mycobacteria-caused diseases is still desired. This the first study aimed at determining activity of two innovative synthetic 1,3,4-oxadiazole molecules, (4-[cyclohexyl(ethyl) sulfamoyl]-N-[5-(furan-2-yl)-1,3,4-oxadiazol-2-yl]benzamide)), namely LMM11, ((N-cyclo-hexyl-N-ethylsulfamoil)-N-(5- (4-fluorophenyl)-1,3,4-oxadiazol-2-il) benzamide), LMM6, against Mycobacterium mycobacteria, their ability present synergism in when...
Aim: To evaluate the potential of three benzohydrazones (1-3), four acylhydrazones derived from isoniazid (INH-acylhydrazones) (4-7) and one hydrazone (8) as antituberculosis agents. Materials & methods: Inhibitory bactericidal activities were determined for reference Mycobacterium tuberculosis (Mtb) strain clinical isolates. Cytotoxicity, drug combinations ethidium bromide accumulation assays also performed. Results: The tested compounds (1-8) presented excellent activity with surprisingly...
Aim: 17 new 4-methoxynaphthalene-N-acylhydrazones were synthesized in order to evaluate their biological action against important pathogens. Methods: In vitro susceptibility assays of compounds performed Paracoccidioides brasiliensis and Mycobacterium tuberculosis. Results: Compounds 4a, 4b 4k the most potent P. brasiliensis, two with minimum inhibitory concentrations ≤1 μg ml-1 exhibited pharmacological synergy amphotericin B. The also showed activity M. tuberculosis, 4c being more...
Chagas' disease is a parasitic infection caused by protozoan Trypanosoma cruzi that affect millions of people worldwide. The available drugs for treatment this cause serious side effects and have variable efficacy, especially in the chronic phase disease. In context, natural compounds shown great potential discovery new chemotherapies various other diseases. present study, we evaluated vitro antiprotozoal activity five species Brazilian Spanish marine sponges (Condrosia reniformes, Tethya...
Aim: To evaluate an assay to detect minimum bactericidal concentration (MBC) in Mycobacterium tuberculosis, using as single model rifampicin, isoniazid, levofloxacin (LVX) and linezolid (LNZ) combination. Material & methods: MBCs were carried out directly from resazurin microtiter plate 3D checkerboard M. tuberculosis H37Rv five resistant clinical isolates. Results: The proposed MBC showed similar values those determined by MGIT™, used control. LVX LNZ's close their MIC values. LNZ or...
Background: Paracoccidioidomycosis (PCM) is a systemic infection caused by Paracoccidioides spp. (Pb). PCM can be associated or clinically confused with tuberculosis (TB), another pulmonary infection, Mycobacterium (Mtb). Futhermore, the long treatment time of TB and cases drug resistance impose difficulties for cure these diseases. Results: New 1,3,4-oxadiazoles containing 4-methoxynaphthalene ring were synthesized their antimicrobial activity was evaluated against Pb Mtb. The derivative 6n...
Aim: To evaluate the activity, cytotoxicity and efflux pumps inhibition of a series 12 novels (-)-camphene-based 1,3,4-thiadiazoles (TDZs) against Mycobacterium tuberculosis (Mtb). Materials & methods: The minimum inhibitory concentration (MIC), for three cell lines, ethidium bromide accumulation checkerboard methods were carried out. Results: Compounds (6a, 6b, 6c, 6g, 6h 6j) showed significant anti-Mtb activity (MIC 3.9-7.8 μg/ml) no antagonism with anti-TB drugs already used in TB...
Tuberculosis is a disease caused by Mycobacterium tuberculosis, with high mortality rates and an extended treatment that causes severe adverse effects, besides the emergence of resistant bacteria. Therefore, search for new compounds anti-M. tuberculosis activity has considerably increased in recent years. In this context, benzohydrazones are significant have antifungal antibacterial action. This study aimed at evaluating vitro 18 against M. tuberculosis. Compounds' cytotoxicity, inhibition...
Background: The treatment of multidrug-resistant tuberculosis (MDR-TB) is a challenge to be overcome. increase resistant isolates associated with serious side effects during therapy leads the search for substances that have anti-TB activity, which make less toxic, and also act in macrophage acidic environment promoted by infection. Objective: aim this study was investigate lapachol β-lapachone activities combination other drugs against Mycobacterium at neutral pH its cytotoxicity. Design:...
Background: The development of drugs is essential to eradicate tuberculosis. Materials & methods: Sixteen 3,5-dinitrobenzoylhydrazone (2–17) derivatives and their synthetic precursors 3,5-dinitrobenzoylhydrazide (1) methyl ester (18) were screened for anti-Mycobacterium tuberculosis (Mtb) potential. Results: Twelve compounds had minimum inhibitory concentration (MIC) ranging from 0.24 7.8 μg/ml against the Mtb strain. activity was maintained in multidrug-resistant clinical isolates. Only...
Background: There is critical need for new therapeutic options treatment of diseases caused by mycobacteria. Materials & methods:Gallesia integrifolia essential oils (EOs) and crude extracts (CEs) were tested their anti-Mycobacterium tuberculosis anti-nontuberculous mycobacteria activity. Results: Minimum inhibitory concentration (MIC) EOs ranged from 15.63 to 62.5 μg/ml against M. >250 nontuberculous CEs showed low All EO demonstrated synergism with antituberculosis drugs. The cytotoxicity...
To evaluate the anti
Aim: To evaluate the modulatory effect of piperine (PIP) on streptomycin (SM) activity in Mycobacterium tuberculosis (Mtb). Materials & methods: SM and PIP minimum inhibitory concentration (MIC) combinatory were determined Mtb H37Rv susceptible resistant clinical isolates. Ethidium bromide accumulation assay relative quantification efflux pumps genes (rv1258c, rv1218c rv2942), after SM+PIP combination exposure, also performed. Results: 25 μg/ml (1/4× MIC) was able to inhibit activity,...
Due to the significant shortage of therapeutic options for carbapenem-resistant Enterobacterales (CRE) infections, new drugs or combinations are urgently required. We show in this study that (−)-camphene-based thiosemicarbazide (TSC) may act synergistically with polymyxin B (PMB) against CRE, rescuing activity antimicrobial. With specific aim a better molecular understanding effect caused by presence TSC, theoretical calculations were also performed study. Based on these findings, it is...
The chemical investigation of Chromolaena palmaris (Sch.Bip. ex Baker) R.M. King & H. Rob. expands the phytochemical composition knowledge genus, since this is first species. Twenty-five compounds were identified, including a phytoprostane, 17 flavonoids, 6 phenolic acids, and caffeoyl-glucoside derivative obtained by classical chromatography UHPLC-HRMS/MS analysis. Moreover, anti-Mycobacterium tuberculosis antiproliferative activities C. evaluated. Dichloromethane fraction showed...