Chimenti Franco, Bizzarri Bruna, Maccioni Elias, Secci Daniela, Bolasco Adriana, Fioravanti Rossella, Chimenti Paola, Granese Arianna, Carradori Simone, Rivanera Daniela, Lilli Daniela, Zicari Alessandra, Distinto Simona
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive Università degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Rome, Italy.
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4635-40. doi: 10.1016/j.bmcl.2007.05.078. Epub 2007 May 27.
In this paper, we report on the synthesis of a novel series of 2-thiazolylhydrazone derivatives and the influence of the substituents on the thiazole ring on antifungal activity. All synthesized compounds were screened for their in vitro activities against 22 clinical isolates of Candida spp., representing six different species, compared to clotrimazole as a reference compound. Some of the tested compounds were found to possess significant antifungal activity when compared to clotrimazole, in particular compound 14 which exhibited higher potency against most of the Candida spp. considered. The compounds that were most active as anti-Candida agents were also submitted to cytotoxic screening by the Trypan Blue dye exclusion assay and in general they were shown to induce low cytotoxic effects.
在本文中，我们报道了一系列新型2-噻唑基腙衍生物的合成以及噻唑环上取代基对其抗真菌活性的影响。与作为参考化合物的克霉唑相比，对所有合成化合物针对22株念珠菌临床分离株（代表6个不同物种）的体外活性进行了筛选。与克霉唑相比，发现一些测试化合物具有显著的抗真菌活性，特别是化合物14，对所考虑的大多数念珠菌物种表现出更高的效力。还通过台盼蓝染料排除试验对作为抗念珠菌剂活性最高的化合物进行了细胞毒性筛选，总体而言，它们显示出低细胞毒性作用。
