Your browser doesn't support javascript.
loading
Exploration of piperazine-derived thioureas as antibacterial and anti-inflammatory agents. In vitro evaluation against clinical isolates of colistin-resistant Acinetobacter baumannii.
Mazzotta, Sarah; Cebrero-Cangueiro, Tania; Frattaruolo, Luca; Vega-Holm, Margarita; Carretero-Ledesma, Marta; Sánchez-Céspedes, Javier; Cappello, Anna Rita; Aiello, Francesca; Pachón, Jerónimo; Vega-Pérez, José Manuel; Iglesias-Guerra, Fernando; Pachón-Ibáñez, María Eugenia.
Affiliation
  • Mazzotta S; Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Seville, E-41071 Seville, Spain; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende (CS), Italy.
  • Cebrero-Cangueiro T; Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain; Institute of Biomedicine of Seville, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain.
  • Frattaruolo L; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende (CS), Italy.
  • Vega-Holm M; Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Seville, E-41071 Seville, Spain. Electronic address: mvegaholm@us.es.
  • Carretero-Ledesma M; Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain; Institute of Biomedicine of Seville, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain.
  • Sánchez-Céspedes J; Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain; Institute of Biomedicine of Seville, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain.
  • Cappello AR; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende (CS), Italy.
  • Aiello F; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende (CS), Italy.
  • Pachón J; Institute of Biomedicine of Seville, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain; Department of Medicine, University of Seville, Seville, Spain.
  • Vega-Pérez JM; Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Seville, E-41071 Seville, Spain. Electronic address: vega@us.es.
  • Iglesias-Guerra F; Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Seville, E-41071 Seville, Spain.
  • Pachón-Ibáñez ME; Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain; Institute of Biomedicine of Seville, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain.
Bioorg Med Chem Lett ; 30(18): 127411, 2020 09 15.
Article in En | MEDLINE | ID: mdl-32717617
ABSTRACT
A. baumannii is one of the most important multidrug-resistant microorganisms in hospital units. It is resistant to many classes of antibiotics and the development of new therapeutic strategies is necessary. The aim of this study was to evaluate the antibacterial activity of a set of piperazine-derived thioureas against 13 clinical strains of colistin-resistant A. baumannii. Six derivatives were identified to inhibit bacterial growth of 46% of the A. baumannii strains at low micromolar concentrations (Minimum Inhibitory Concentration from 1.56 to 6.25 µM). A common structural feature in most active compounds was the presence of a 3,5-bis-trifluoromethyl phenyl ring at the thiourea function. In addition, the ability of the compounds to inhibit production of nitric oxide (NO) was examined in RAW 264.7 murine macrophages, highlighting the potential of piperazine-derived thioureas as promising scaffolds for the design of new combined anti-bacterial/anti-inflammatory agents.
Subject(s)
Key words
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Piperazines / Thiourea / Acinetobacter Infections / Colistin / Acinetobacter baumannii / Anti-Inflammatory Agents / Anti-Bacterial Agents Limits: Animals / Humans Language: En Year: 2020 Type: Article
Fulltext
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Piperazines / Thiourea / Acinetobacter Infections / Colistin / Acinetobacter baumannii / Anti-Inflammatory Agents / Anti-Bacterial Agents Limits: Animals / Humans Language: En Year: 2020 Type: Article