Pricopie Andreea-Iulia, Ionuț Ioana, Marc Gabriel, Arseniu Anca-Maria, Vlase Laurian, Grozav Adriana, Găină Luiza Ioana, Vodnar Dan C, Pîrnău Adrian, Tiperciuc Brîndușa, Oniga Ovidiu
Department of Pharmaceutical Chemistry, "Iuliu Hațieganu" University of Medicine and Pharmacy, 41 Victor Babeș Street, 400012 Cluj-Napoca, Romania.
Preclinic Department, Pharmacy Specialization, Faculty of Medicine, Lucian Blaga University of Sibiu, 2A Lucian Blaga Street, 550169 Sibiu, Romania.
Molecules. 2019 Sep 21;24(19):3435. doi: 10.3390/molecules24193435.
In the context of there being a limited number of clinically approved drugs for the treatment of sp.-based infections, along with the rapid development of resistance to the existing antifungals, two novel series of 4-phenyl-1,3-thiazole and 2-hydrazinyl-4-phenyl-1,3-thiazole derivatives were synthesized and tested in vitro for their anti- potential. Two compounds ( and ) showed promising inhibitory activity against the pathogenic strain, exhibiting substantially lower MIC values (7.81 μg/mL and 3.9 μg/mL, respectively) as compared with the reference drug fluconazole (15.62 μg/mL). Their anti- activity is also supported by molecular docking studies, using the fungal lanosterol C14α-demethylase as the target enzyme. The interaction of the most biologically active synthesized compound with bovine serum albumin was investigated through fluorescence spectroscopy, and the obtained data suggested that this molecule might efficiently bind carrier proteins in vivo in order to reach the target site.
鉴于用于治疗基于sp.的感染的临床批准药物数量有限，以及现有抗真菌药物耐药性的迅速发展，合成了两个新型系列的4-苯基-1,3-噻唑和2-肼基-4-苯基-1,3-噻唑衍生物，并在体外测试了它们的抗真菌潜力。两种化合物（和）对致病菌株显示出有前景的抑制活性，与参考药物氟康唑（15.62μg/mL）相比，其最低抑菌浓度值显著更低（分别为7.81μg/mL和3.9μg/mL）。以真菌羊毛甾醇C14α-脱甲基酶为靶酶的分子对接研究也支持了它们的抗真菌活性。通过荧光光谱研究了最具生物活性的合成化合物与牛血清白蛋白的相互作用，所得数据表明该分子可能在体内有效地结合载体蛋白以到达靶位点。
