期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 4, 期 9, 页码 852-857出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml400187w
关键词
Antifungal; amidinourea; macrocyclization; ring-closing metathesis; Candida species; fluconazole; antifungal drug-resistance
资金
- Bakker Medical S.r.l.
- University of Siena
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.
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