Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.

Fabrizio Manetti; Daniele Castagnolo; Francesco Raffi; Alessandra Zizzari; Suvi Rajamäki; Silvia D’Arezzo; Paolo Visca; Alessandra Cona; Maria Enrica Fracasso; Denise Doria; Brunella Posteraro; Maurizio Sanguinetti; Giovanni Fadda; Maurizio Botta

doi:10.1021/jm900760k

Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.

Fabrizio Manetti, Daniele Castagnolo, Francesco Raffi, Alessandra Zizzari, Suvi Rajamäki, Silvia D’Arezzo, Paolo Visca, Alessandra Cona, Maria Enrica Fracasso, Denise Doria, Brunella Posteraro, Maurizio Sanguinetti, Giovanni Fadda, Maurizio Botta

Northumbria University

Research output: Contribution to journal › Article › peer-review

56 Citations (Scopus)

Abstract

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 in the micromolar range and a biological activity profile in 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.

Original language	English
Pages (from-to)	7376-7379
Journal	Journal of Medicinal Chemistry
Volume	52
Issue number	23
DOIs	https://doi.org/10.1021/jm900760k
Publication status	Published - 2009

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Manetti, F., Castagnolo, D., Raffi, F., Zizzari, A., Rajamäki, S., D’Arezzo, S., Visca, P., Cona, A., Fracasso, M. E., Doria, D., Posteraro, B., Sanguinetti, M., Fadda, G., & Botta, M. (2009). Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp. Journal of Medicinal Chemistry, 52(23), 7376-7379. https://doi.org/10.1021/jm900760k

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title = "Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.",

abstract = "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 in the micromolar range and a biological activity profile in 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.",

author = "Fabrizio Manetti and Daniele Castagnolo and Francesco Raffi and Alessandra Zizzari and Suvi Rajam{\"a}ki and Silvia D{\textquoteright}Arezzo and Paolo Visca and Alessandra Cona and Fracasso, {Maria Enrica} and Denise Doria and Brunella Posteraro and Maurizio Sanguinetti and Giovanni Fadda and Maurizio Botta",

year = "2009",

doi = "10.1021/jm900760k",

language = "English",

volume = "52",

pages = "7376--7379",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "23",

}

Manetti, F, Castagnolo, D, Raffi, F, Zizzari, A, Rajamäki, S, D’Arezzo, S, Visca, P, Cona, A, Fracasso, ME, Doria, D, Posteraro, B, Sanguinetti, M, Fadda, G & Botta, M 2009, 'Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.', Journal of Medicinal Chemistry, vol. 52, no. 23, pp. 7376-7379. https://doi.org/10.1021/jm900760k

TY - JOUR

T1 - Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.

AU - Manetti, Fabrizio

AU - Castagnolo, Daniele

AU - Raffi, Francesco

AU - Zizzari, Alessandra

AU - Rajamäki, Suvi

AU - D’Arezzo, Silvia

AU - Visca, Paolo

AU - Cona, Alessandra

AU - Fracasso, Maria Enrica

AU - Doria, Denise

AU - Posteraro, Brunella

AU - Sanguinetti, Maurizio

AU - Fadda, Giovanni

AU - Botta, Maurizio

PY - 2009

Y1 - 2009

N2 - 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 in the micromolar range and a biological activity profile in 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.

AB - 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 in the micromolar range and a biological activity profile in 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.

U2 - 10.1021/jm900760k

DO - 10.1021/jm900760k

M3 - Article

SN - 0022-2623

VL - 52

SP - 7376

EP - 7379

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 23

ER -

Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.

Abstract

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