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

被引：55
|
作者：
Manetti, Fabrizio [1 ]
Castagnolo, Daniele [1 ]
Raffi, Francesco [1 ]
Zizzari, Alessandra T. [1 ]
Rajamaki, Suvi [1 ]
D'Arezzo, Silvia [2 ]
Visca, Paolo [2 ,3 ]
Cona, Alessandra [3 ]
Fracasso, Maria Enrica [4 ]
Doria, Denise [4 ]
Posteraro, Brunella [5 ]
Sanguinetti, Maurizio [5 ]
Fadda, Giovanni [5 ]
Botta, Maurizio [1 ]
机构：
[1] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy
[2] Natl Inst Infect Dis Lazzaro Spallanzani IRCCS, Rome, Italy
[3] Univ Roma Tre, Dept Biol, I-00146 Rome, Italy
[4] Univ Verona, Dept Med & Publ Hlth, Pharmacol Sect, I-37100 Verona, Italy
[5] Univ Cattolica Sacro Cuore, Ist Microbiol, I-00168 Rome, Italy
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 23期
关键词：
CONVERSION; THERAPY;
D O I：
10.1021/jm900760k
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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.
引用
收藏
页码：7376 / 7379
页数：4
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