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.

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页码：7376 / 7379

页数：4

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