新型线性胍类和大环脒基脲衍生物的合成，这些衍生物对念珠菌属和曲霉属具有高抗真菌活性。
Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.
作者信息
Manetti Fabrizio, Castagnolo Daniele, Raffi Francesco, Zizzari Alessandra T, Rajamäki Suvi, D'Arezzo Silvia, Visca Paolo, Cona Alessandra, Fracasso Maria Enrica, Doria Denise, Posteraro Brunella, Sanguinetti Maurizio, Fadda Giovanni, Botta Maurizio
机构信息
Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via Alcide de Gasperi 2, I-53100 Siena, Italy.
出版信息
J Med Chem. 2009 Dec 10;52(23):7376-9. doi: 10.1021/jm900760k.
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.
合成了新型线性和环状胍，并在体外测试了它们对念珠菌属临床相关菌株的抗真菌活性，与氟康唑进行比较。大环化合物显示出微摩尔范围内的最低抑菌浓度，在某些情况下其生物活性谱优于氟康唑。还对一种大环衍生物针对曲霉菌种进行了测试，其显示出与两性霉素B和伊曲康唑相当的高抗真菌活性。
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