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New Teixobactin Analogues with a Total Lactam Ring.
Scioli, Giuseppe; Marinaccio, Lorenza; Bauer, Marta; Kamysz, Wojciech; Parmar, Anish; Newire, Enas; Singh, Ishwar; Stefanucci, Azzurra; Mollica, Adriano.
Afiliación
  • Scioli G; Department of Pharmacy, University "G. d'Annunzio" Chieti-Pescara, Via dei Vestini 31, 66100 Chieti, Italy.
  • Marinaccio L; Department of Pharmacy, University "G. d'Annunzio" Chieti-Pescara, Via dei Vestini 31, 66100 Chieti, Italy.
  • Bauer M; Department of Inorganic Chemistry, Faculty of Pharmacy, Medical University of Gdansk, 80-416 Gdansk, Poland.
  • Kamysz W; Department of Inorganic Chemistry, Faculty of Pharmacy, Medical University of Gdansk, 80-416 Gdansk, Poland.
  • Parmar A; Antimicrobial Pharmacodynamics and Therapeutics, Department of Molecular and Clinical Pharmacology, University of Liverpool, Sherrington Building, L69 3GA Liverpool, U.K.
  • Newire E; Department of Chemistry, The Robert Robinson Laboratories, The University of Liverpool, L69 3BX Liverpool, United Kingdom.
  • Singh I; Antimicrobial Pharmacodynamics and Therapeutics, Department of Molecular and Clinical Pharmacology, University of Liverpool, Sherrington Building, L69 3GA Liverpool, U.K.
  • Stefanucci A; Department of Chemistry, The Robert Robinson Laboratories, The University of Liverpool, L69 3BX Liverpool, United Kingdom.
  • Mollica A; Antimicrobial Pharmacodynamics and Therapeutics, Department of Molecular and Clinical Pharmacology, University of Liverpool, Sherrington Building, L69 3GA Liverpool, U.K.
ACS Med Chem Lett ; 14(12): 1827-1832, 2023 Dec 14.
Article en En | MEDLINE | ID: mdl-38116416
ABSTRACT
Teixobactin is a new antibiotic peptide with strong efficacy against several Gram-positive resistant bacteria, the structure of which is extremely difficult to obtain in the laboratory via multistep conventional synthesis. To face the increasing antibiotic resistant bacteria, it is fundamental to introduce new types of antibiotics with innovative mechanisms of action without resistance; thus, many scientists are studying and developing new methods to synthesize teixobactin analogues. In this work, seven Arg10-teixobactin analogues with a total lactam ring have been prepared via solid phase peptide synthesis. In order to obtain the total lactam ring, d-Thr8 was replaced by (2R,3S)-diamino-propionic acid. To verify their antimicrobial activity and efficacy, each analogue was tested with MIC against different resistant pathogens, showing an interesting activity for Nle11 containing compounds.

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2023 Tipo del documento: Article País de afiliación: Italia

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2023 Tipo del documento: Article País de afiliación: Italia