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Home / Archives for Pieroni M

Sodium hyaluronate nanocomposite respirable microparticles to tackle antibiotic resistance with potential application in treatment of mycobacterial pulmonary infections

  • Authors: Rossi I, Buttini F, Sonvico F, Affaticati F, Martinelli F, Annunziato G, Machado D, Viveiros M, Pieroni M, Bettini R
  • Publication Year: 2019
  • Journal: Pharmaceutics
  • Link: https://www.ncbi.nlm.nih.gov/pubmed/31052403

Tuberculosis resistant cases have been estimated to grow every year. Besides Mycobacterium tuberculosis, other mycobacterial species are responsible for an increasing number of difficult-to-treat infections. To increase efficacy of pulmonary treatment of mycobacterial infections an inhalable antibiotic powder targeting infected alveolar macrophages (AMs) and including an efflux pump inhibitor was developed. Low molecular weight sodium hyaluronate […]
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Adjuvant therapies against tuberculosis: Discovery of a 2-aminothiazole targeting Mycobacterium tuberculosis energetics

  • Authors: Machado D, Azzali E, Couto I, Costantino G, Pieroni M, Viveiros M
  • Publication Year: 2018
  • Journal: Future Microbiology
  • Link: https://www.futuremedicine.com/doi/10.2217/fmb-2018-0110

AIM: To evaluate the activity of the 2-aminothiazole UPAR-174 following an unexplored approach: targeting Mycobacterium tuberculosis with lipophilic compounds that present antituberculosis and efflux inhibitory activity. METHODS: Antituberculosis activity was assessed against replicating, nonreplicating and intracellular bacilli. Its capacity to inhibit active efflux was determined. ATP quantification and membrane potential analysis were performed. Intracellular activity […]
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Challenging the drug-likeness dogma for new drug discovery in Tuberculosis

  • Authors: Machado D, Girardini M, Viveiros M, Pieroni M
  • Publication Year: 2018
  • Journal: Frontiers in Microbiology
  • Link: https://www.ncbi.nlm.nih.gov/pubmed/30018597

The emergence of multi- and extensively drug resistant tuberculosis worldwide poses a great threat to human health and highlight the need to discover and develop new, effective and inexpensive antituberculosis agents. High-throughput screening assays against well-validated drug targets and structure based drug design have been employed to discover new lead compounds. However, the great majority […]
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Efflux Activity Differentially Modulates the Levels of Isoniazid and Rifampicin Resistance among Multidrug Resistant and Monoresistant Mycobacterium tuberculosis Strains

  • Authors: Machado D, Perdigão J, Portugal I, Pieroni M, Silva PA, Couto I, Viveiros M
  • Publication Year: 2018
  • Journal: Antibiotics
  • Link: http://www.mdpi.com/2079-6382/7/1/18/htm

With the growing body of knowledge on the contribution of efflux activity toMycobacterium tuberculosisdrug resistance, increased attention has been given to the use of efflux inhibitors as adjuvants of tuberculosis therapy. Here, we investigated how efflux activity modulates the levels of efflux between monoresistant and multi- and extensively drug resistant (M/XDR)M. tuberculosisclinical isolates. The strains […]
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Substituted N-Phenyl-5-(2-(phenylamino)thiazol-4-yl)isoxazole-3-carboxamides Are Valuable Antitubercular Candidates that Evade Innate Efflux Machinery

  • Authors: Azzali E, Cabassi CS, Costantino G, Flisi S, Kaushik A, Lamichhane G, Machado D, Pieroni M, Vacondio F, Viveiros M
  • Publication Year: 2017
  • Journal: Journal of Medicinal Chemistry
  • Link: https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b00793

Tuberculosis remains one of the deadliest infectious diseases in the world, and the increased number of multidrug-resistant and extremely drug-resistant strains is a significant reason for concern. This makes the discovery of novel antitubercular agents a cogent priority. We have previously addressed this need by reporting a series of substituted 2-aminothiazoles capable to inhibit the […]
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About GHTM

GHTM is a R&D Unit that brings together researchers with a track record in Tropical Medicine and International & Global Health. It aims at strengthening Portugal's role as a leading partner in the development and implementation of a global health research agenda. Our evidence-based interventions contribute to the promotion of equity in health and to improve the health of populations.

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