Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
Eur J Med Chem. 2013 Jul;65:102-11. doi: 10.1016/j.ejmech.2013.04.042. Epub 2013 May 1.
Thirty-eight new (4-(4-substituted-phenyl/2,4-disubstituted-phenyl)-thiazol-2-yl)hydrazine derivatives were synthesized in good yield and assayed for their in vitro anti-Candida activity, compared to topical and systemic antifungal drugs, against twenty-two clinical isolates of Candida spp. The concurrent presence of aliphatic chains or cycloaliphatic rings at N1-hydrazine and a 4-methyl/4-methoxyphenyl at C4 position of the thiazole nucleus exhibited an interesting anti-Candida inhibitory activity. Moreover, some of the most active compounds showed synergistic antifungal effects and lower cell toxicity when combined with clotrimazole.
合成了 38 种新型(4-(4-取代苯基/2,4-二取代苯基)-噻唑-2-基)肼衍生物,并对其进行了体外抗念珠菌活性测定,与局部和全身抗真菌药物进行了比较,共对 22 株临床分离的念珠菌属进行了测定。N1-肼中同时存在脂肪链或环脂肪环,噻唑核的 C4 位置为 4-甲基/4-甲氧基苯基,表现出有趣的抗念珠菌抑制活性。此外,一些最有效的化合物与克霉唑联合使用时,表现出协同的抗真菌作用和较低的细胞毒性。