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Synthesis of New Linear Guanidines and Macrocyclic Amidinourea Derivatives Endowed with High Antifungal Activity against Candida spp. and Aspergillus spp.

  作者 MANETTI FABRIZIO; CASTAGNOLO DANIELE; RAFFI FRANCESCO; ZIZZARI ALESSANDRA T; RAJAMAKI SUVI; DAREZZO SILVIA; VISCA PAOLO; CONA ALESSANDRA; FRACASSO MARIA ENRICA; DORIA DENISE; POSTERARO BRUNELLA; SANGUINETTI MAURIZIO; FADDA GIOVANNI; BOTTA MAURIZIO  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2009年52-23;  页码  7376-7379  
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[摘要]New linear and Cyclic guanidines were synthesized and tested in vitro for their antifungal activity toward clinically relevant strains of Candida species, in comparison to fluconazole. Macrocyclic Compounds showed a minimum inhibitory concentration ill the micromolar range and a biological activity profile ill some cases better than that of fluconazole. One macrocyclic derivative was also tested against Aspergillus species and showed high antifungal activity comparable to that of amphotericin B and itraconazole.

 
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