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

页码：7376 / 7379

页数：4

共 16 条

[11] Novel triazole antifungal agents
Hoffman, HL
Ernst, EJ
Klepser, ME
[J]. EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2000, 9 (03) : 593 - 605
[12] Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents
Jana, GH
Jain, S
Arora, SK
Sinha, N
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2005, 15 (15) : 3592 - 3595
[13] Candida resistance and its clinical relevance
Klepser, Michael E.
[J]. PHARMACOTHERAPY, 2006, 26 (06): : 68S - 75S
[14] Topical therapy for fungal infections
Kyle, AA
Dahl, MV
[J]. AMERICAN JOURNAL OF CLINICAL DERMATOLOGY, 2004, 5 (06) : 443 - 451
[15] MECHANISM OF CONVERSION TO MUCOIDY IN PSEUDOMONAS-AERUGINOSA INFECTING CYSTIC-FIBROSIS PATIENTS
MARTIN, DW
SCHURR, MJ
MUDD, MH
GOVAN, JRW
HOLLOWAY, BW
DERETIC, V
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (18) : 8377 - 8381
[16] Anticandidal low molecular compounds from higher plants with special reference to compounds from essential oils
Pauli, A
[J]. MEDICINAL RESEARCH REVIEWS, 2006, 26 (02) : 223 - 268

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