Discovery of Substituted (2-Aminooxazol-4-yl)Isoxazole-3-carboxylic Acids as Inhibitors of Bacterial Serine Acetyltransferase in the Quest for Novel Potential Antibacterial Adjuvants.

adjuvant therapies antimicrobial resistance cysteine biosynthesis non-essential targets serine acetyltransferase

Journal

Pharmaceuticals (Basel, Switzerland)
ISSN: 1424-8247
Titre abrégé: Pharmaceuticals (Basel)
Pays: Switzerland
ID NLM: 101238453

Informations de publication

Date de publication:
23 Feb 2021
Historique:
received: 26 01 2021
revised: 15 02 2021
accepted: 19 02 2021
entrez: 6 3 2021
pubmed: 7 3 2021
medline: 7 3 2021
Statut: epublish

Résumé

Many bacteria and actinomycetales use L-cysteine biosynthesis to increase their tolerance to antibacterial treatment and establish a long-lasting infection. In turn, this might lead to the onset of antimicrobial resistance that currently represents one of the most menacing threats to public health worldwide. The biosynthetic machinery required to synthesise L-cysteine is absent in mammals; therefore, its exploitation as a drug target is particularly promising. In this article, we report a series of inhibitors of

Identifiants

pubmed: 33672408
pii: ph14020174
doi: 10.3390/ph14020174
pmc: PMC7931047
pii:
doi:

Types de publication

Journal Article

Langues

eng

Subventions

Organisme : Academy of Finland
ID : 277001

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Auteurs

Joana Magalhães (J)

P4T Group, Department of Food and Drug, University of Parma, 43124 Parma, Italy.

Nina Franko (N)

Laboratory of Biochemistry and Molecular Biology, Department of Food and Drug, University of Parma, 43124 Parma, Italy.

Samanta Raboni (S)

Laboratory of Biochemistry and Molecular Biology, Department of Food and Drug, University of Parma, 43124 Parma, Italy.
Institute of Biophysics, CNR, 56124 Pisa, Italy.

Giannamaria Annunziato (G)

P4T Group, Department of Food and Drug, University of Parma, 43124 Parma, Italy.
Centro Interdipartimentale Misure (CIM) 'G. Casnati', University of Parma, 43124 Parma, Italy.

Päivi Tammela (P)

Drug Research Program, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, P.O. Box 56 (Viikinkaari 5 E), FI-00014 Helsinki, Finland.

Agostino Bruno (A)

P4T Group, Department of Food and Drug, University of Parma, 43124 Parma, Italy.

Stefano Bettati (S)

Institute of Biophysics, CNR, 56124 Pisa, Italy.
Department of Medicine and Surgery, University of Parma, Via Volturno, 39, 43125 Parma, Italy.
National Institute of Biostructures and Biosystems, 00136 Rome, Italy.

Stefano Armao (S)

Laboratory of Biochemistry and Molecular Biology, Department of Food and Drug, University of Parma, 43124 Parma, Italy.

Costanza Spadini (C)

Operative Unit of Animals Infectious Diseases, Department of Veterinary Science, University of Parma, Via del Taglio 10, 43126 Parma, Italy.

Clotilde Silvia Cabassi (CS)

Operative Unit of Animals Infectious Diseases, Department of Veterinary Science, University of Parma, Via del Taglio 10, 43126 Parma, Italy.

Andrea Mozzarelli (A)

Laboratory of Biochemistry and Molecular Biology, Department of Food and Drug, University of Parma, 43124 Parma, Italy.
Institute of Biophysics, CNR, 56124 Pisa, Italy.
National Institute of Biostructures and Biosystems, 00136 Rome, Italy.

Marco Pieroni (M)

P4T Group, Department of Food and Drug, University of Parma, 43124 Parma, Italy.
Centro Interdipartimentale Misure (CIM) 'G. Casnati', University of Parma, 43124 Parma, Italy.

Barbara Campanini (B)

Laboratory of Biochemistry and Molecular Biology, Department of Food and Drug, University of Parma, 43124 Parma, Italy.

Gabriele Costantino (G)

P4T Group, Department of Food and Drug, University of Parma, 43124 Parma, Italy.
Centro Interdipartimentale Misure (CIM) 'G. Casnati', University of Parma, 43124 Parma, Italy.

Classifications MeSH