Novel macrocyclic amidinoureas: Potent non-azole antifungals active against wild-type and resistant Candida species

Maurizio Sanguinetti, Brunella Posteraro, Stefania Sanfilippo, Daniele Castagnolo, Dominique Sanglard, Giovanni Donzellini, Maurizio Botta

Risultato della ricerca: Contributo in rivistaArticolo in rivista

18 Citazioni (Scopus)

Abstract

Novel macrocyclic amidinourea derivatives 11, 18, and 25 were synthesized and evaluated as antifungal agents against wild-type and fluconazole resistant Candida species. Macrocyclic compounds 11 and 18 were synthesized through a convergent approach using as a key step a ring-closing metathesis macrocyclization reaction, whereas compounds 25 were obtained by our previously reported synthetic pathway. All the macrocyclic amidinoureas showed antifungal activity toward different Candida species higher or comparable to fluconazole and resulted highly active against fluconazole resistant Candida strains showing in many cases minimum inhibitory concentration values lower than voriconazole. © 2013 American Chemical Society.
Lingua originaleEnglish
pagine (da-a)852-857
Numero di pagine6
RivistaACS Medicinal Chemistry Letters
Volume4
DOI
Stato di pubblicazionePubblicato - 2013

Keywords

  • Antifungal
  • Biochemistry
  • Candida species
  • Drug Discovery3003 Pharmaceutical Science
  • Organic Chemistry
  • amidinourea
  • antifungal drug-resistance
  • fluconazole
  • macrocyclization
  • ring-closing metathesis

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