A5019545326- Tuberculosis Research and Epidemiology
- Cancer therapeutics and mechanisms
- Microbial Natural Products and Biosynthesis
- Biochemical and Molecular Research
- Mycobacterium research and diagnosis
- Plant chemical constituents analysis
- Berberine and alkaloids research
- Quinazolinone synthesis and applications
- Synthesis and Biological Activity
- Antibiotic Resistance in Bacteria
- Advanced Drug Delivery Systems
- Phenothiazines and Benzothiazines Synthesis and Activities
- Phytochemistry and Bioactive Compounds
- Alkaloids: synthesis and pharmacology
- Phytochemistry and Biological Activities
- Bacterial Genetics and Biotechnology
- Bioactive Compounds and Antitumor Agents
- Synthesis and Reactivity of Heterocycles
- Microwave-Assisted Synthesis and Applications
- Probiotics and Fermented Foods
Universidad de Zaragoza
2011-2022
Instituto de Salud Carlos III
2017-2022
Centro de Investigación Biomédica en Red de Enfermedades Respiratorias
2011-2022
Instituto de Investigación Sanitaria Aragón
2018-2022
Spectinamides are a novel class of antitubercular agents with the potential to treat drug-resistant tuberculosis infections. Their activity is derived from both ribosomal affinity and their ability overcome intrinsic efflux mediated by Mycobacterium Rv1258c pump. This study explores structure-activity relationships through analysis 50 targeted spectinamides. Compounds evaluated for translational inhibition, MIC in pump deficient wild type strains, efficacy an acute model infection. The...
The increasing incidence of multidrug-resistant Mycobacterium tuberculosis strains and the very few drugs available for treatment are promoting discovery development new molecules that could help in control this disease. Bacteriocin AS-48 is an antibacterial peptide produced by Enterococcus faecalis active against several Gram-positive bacteria. We have found was tuberculosis, including H37Rv other reference clinical strains, also some nontuberculous mycobacterial species. combination with...
The increase of bacterial strains resistant to most the available antibiotics shows a need explore novel antibacterial targets discover antimicrobial drugs. Bifunctional FAD synthetases (FADSs) synthesise flavin mononucleotide (FMN) and adenine dinucleotide (FAD). These cofactors act in vital processes as part flavoproteins, making FADS an essential enzyme. Bacterial FADSs are potential because differences mammalian enzymes, particularly at producing site. We have optimised activity-based...
In recent years, thymidylate kinase (TMPK), an enzyme indispensable for bacterial DNA biosynthesis, has been pursued the development of new antibacterial agents including against Mycobacterium tuberculosis, causative agent widespread infectious disease tuberculosis (TB). response to a growing need more effective anti-TB drugs, we have built upon our previous efforts toward exploration novel and potent TMPK (MtTMPK) inhibitors, reported here design series non-nucleoside inhibitors MtTMPK. The...
Aim: Production of Matryoshka-type gastroresistant microparticles containing antibiotic-loaded poly lactic-co-glycolic acid (PLGA) nanoparticles (NP) against Mycobacterium tuberculosis. Materials & methods: The emulsification and evaporation methods were followed for the synthesis PLGA–NPs methacrylic acid-ethyl acrylate-based coatings to protect rifampicin from degradation under simulated gastric conditions. Results conclusion: inner NPs here reported can be released intestinal conditions...
The therapeutic potential of 3H-pyrrolo[2,3-c]quinolines-the main core Marinoquinoline natural products-has been explored for the development new anti-TB agents. chemical modification various positions in this scaffold has led to discovery two pyrroloquinolines (compounds 50 and 54) with good vitro activity against virulent strains Mycobacterium tuberculosis (H37Rv, MIC = 4.1 μM 4.2 μM, respectively). Enzymatic assays showed that both derivatives are inhibitors glutamate-5-kinase (G5K,...
The spread of multidrug-resistant isolates Mycobacterium tuberculosis requires the discovery new drugs directed to targets. In this study, we investigated activity two boldine-derived alkaloids, seconeolitsine (SCN) and N-methyl-seconeolitsine (N-SCN), against M. tuberculosis. These compounds have been shown target DNA topoisomerase I enzyme inhibit growth Streptococcus pneumoniae. Both SCN N-SCN inhibited at 1.95 15.6 microM, depending on strain. smegmatis inhibitory effect correlated with...
A number of medicinal plants have long been used by traditional healers to treat tuberculosis and related diseases in Mozambique [1,2]. The present study was aimed evaluate selected for their vitro antimycobacterial activity, reveal the main classes compounds which might account observed activity. Four organic solvents (n-hexane, dichloromethane, ethylacetate, 70% ethanol) were sequential extraction. Decoction each plant material prepared according use. Different species mycobacteria,...
Semi-synthesis of natural products has been considered to be an optional method for providing more active and less toxic derivatives establishment structure-activity relationships (SAR). The genus Zanthoxylum is a rich source benzophenanthridine-type alkaloids. In our search antimycobacterial constituents from medicinal plants, we have extensively investigated the African plant capense, which led isolation twenty-seven compounds most them Benzophenanthridine alkaloids were found various...
Mycobacterium tuberculosis infects about one-third of the world's population, and causes almost 2 million deaths annually. In 2007, there were 9.27 new TB cases. Despite more than 40 years anti-TB chemotherapy, remains one leading infectious diseases worldwide. The association with HIV epidemic, increasing emergence multi-drug resistant (MDR-TB) extensively drug-resistant (XDR-TB) make virtually untreatable available drugs [1–3]. From this point, is evidently an urgent need to develop...
One approach to identify potential anti-tuberculosis drug leads is screen medicinal plants traditionally used for tuberculosis treatment. By bioassay-guided fractionation, sixteen compounds, with various structural features, were isolated from the roots of African plant Zanthoxylum capense (Thunb.) Harv., which by traditional healers in Mozambique treat TB patients. The compounds evaluated antimycobacterial activity against different M. strains as well cytotoxicity towards THP-1 macrophages....