Opletalova Veronika, Dolezel Jan, Kunes Jiri, Buchta Vladimir, Vejsova Marcela, Kucerova-Chlupacova Marta
Department of Pharmaceutical Chemistry and Pharmaceutical Analysis, Faculty of Pharmacy in Hradec Kralove, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic.
GlaxoSmithKline, Hvezdova 1734/2c, 140 00 Prague, Czech Republic.
Molecules. 2016 Nov 23;21(11):1592. doi: 10.3390/molecules21111592.
Two novel thiosemicarbazones and eight novel 2-{[1-(5-alkyl/arylalkylpyrazin-2-yl)ethylidene]hydrazono}-1,3-thiazolidin-4-ones were prepared and tested against a panel of eight fungal strains- ATCC 44859, 156, E 28, 20/I, 1188, 231, 272, and 445. 1,3-Thiazolidin-4-ones exhibited activity against all strains, the most potent derivative was 2-{[1-(5-butylpyrazin-2-yl)ethylidene]hydrazono}e-1,3-thiazolidin-4-one. Susceptibility of to the studied 1,3-thiazolidin-4-ones (minimum inhibitory concentrations (MICs) were in the range 0.57 to 2.78 mg/L) is of great interest as this opportunistic pathogen is poorly susceptible to azoles and becomes resistant to echinocandins. Antifungal potency of thiosemicarbazones was slightly lower than that of 1,3-thiazolidin-4-ones.
制备了两种新型硫代氨基脲和八种新型2-{[1-(5-烷基/芳基烷基吡嗪-2-基)亚乙基]肼基}-1,3-噻唑烷-4-酮，并针对八种真菌菌株（ATCC 44859、156、E 28、20/I、1188、231、272和445）进行了测试。1,3-噻唑烷-4-酮对所有菌株均表现出活性，最有效的衍生物是2-{[1-(5-丁基吡嗪-2-基)亚乙基]肼基}-1,3-噻唑烷-4-酮。由于这种机会致病菌对唑类药物敏感性较差且对棘白菌素产生耐药性，因此其对所研究的1,3-噻唑烷-4-酮的敏感性（最低抑菌浓度（MICs）在0.57至2.78 mg/L范围内）备受关注。硫代氨基脲的抗真菌效力略低于1,3-噻唑烷-4-酮。
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