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Design and Synthesis of Novel 13-Thiazole and 2-Hydrazinyl-13-Thiazole Derivatives as Anti-Candida Agents: In Vitro Antifungal Screening Molecular Docking Study and Spectroscopic Investigation of their Binding Interaction with Bovine Serum Albumin

机译：新型13-噻唑和2-肼基-13-噻唑衍生物作为抗念珠菌药物的设计与合成：体外抗真菌筛选分子对接研究以及与牛血清白蛋白结合相互作用的光谱研究

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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.

机译：在治疗基于sp。的感染的临床批准药物数量有限的情况下，随着对现有抗真菌药耐药性的迅速发展，出现了两个新的4-苯基-1,3-噻唑和2合成了-肼基-4-苯基-1,3-噻唑衍生物，并在体外测试了其抗电势。与参考药物氟康唑（15.62μg/ mL）相比，两种化合物（和）对病原体菌株显示出有希望的抑制活性，其MIC值分别低得多（分别为7.81μg/ mL和3.9μg/ mL）。使用真菌羊毛甾醇C14α-脱甲基酶作为目标酶，分子对接研究还支持了它们的抗活性。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，获得的数据表明该分子可能在体内有效结合载体蛋白以到达靶位点。

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期刊名称 Molecules
作者
Andreea-Iulia Pricopie; Ioana Ionuț; Gabriel Marc; Anca-Maria Arseniu; Laurian Vlase; Adriana Grozav; Luiza Ioana Găină; Dan C. Vodnar; Adrian Pîrnău; Brîndușa Tiperciuc; Ovidiu Oniga;
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年(卷),期 2019(24),19
年度 2019
页码 -1
总页数 21
原文格式 PDF
正文语种
中图分类分子生物学;
关键词
13-thiazole; anti-;

机译：13-噻唑;抗;

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专利

1. Synthesis of a Novel Hydrazone Derivative and Biophysical Studies of Its Interactions with Bovine Serum Albumin by Spectroscopic, Electrochemical, and Molecular Docking Methods [J] . Fang-Fang Tian, Feng-Lei Jiang, Xiao-Le Han The journal of physical chemistry, B. Condensed matter, materials, surfaces, interfaces & biophysical . 2010,第46期

机译：新型Hy衍生物的合成及其与牛血清白蛋白相互作用的生物物理的光谱，电化学和分子对接方法研究
2. In vitro study on binding interaction of quinapril with bovine serum albumin (BSA) using multi-spectroscopic and molecular docking methods [J] . Shi Jie-hua, Pan Dong-qi, Jiang Min, Journal of Biomolecular Structure and Dynamics . 2017,第9a10期

机译：用多光谱和分子对接方法在体外研究Quinapril与牛血清白蛋白（BSA）的结合相互作用
3. Binding interaction of an anionic amino acid surfactant with bovine serum albumin: physicochemical and spectroscopic investigations combined with molecular docking study [J] . Dasmandal Somnath, Kundu Arjama, Rudra Suparna, RSC Advances . 2015,第96期

机译：阴离子氨基酸表面活性剂与牛血清白蛋白的结合相互作用：物理化学和光谱研究结合分子对接研究
4. In Vitro Study of Ethyl-4-(3,4.5-trimethoxyphenyl)-2,7,7- trimethyl-5-oxo1,4,5,6,7,8-hexahydroquinoline-3-carboxylate and Bovine Serum Albumin Using Multi-Spectroscopic Techniques and Molecular Docking [C] . Sunil D. Kumbhar, Anil H. Gore, Prafulla B. Choudhari International Conference on Advances in Materials Science . 2019

机译：乙基-4-（3,4.5-三甲氧基苯基）-2,7,7-三甲基-5-氧代1,4,5,6,7,8-六羟基喹啉-3-羧酸盐和牛血清白蛋白使用多重的体外研究光谱技术和分子对接
5. Part I. Synthesis of lipid A derivatives and their interactions with lipid A binding agents. Part II. Synthesis of glycosphingolipids to study natural killer T cell stimulation. [D] . Yin, Ning. 2005

机译：第一部分：脂质A衍生物的合成及其与脂质A结合剂的相互作用。第二部分合成鞘糖脂以研究自然杀伤性T细胞刺激。
6. Study of the Interactions of Bovine Serum Albumin with the New Anti-Inflammatory Agent 4-(13-Dioxo-13-dihydro-2H-isoindol-2-yl)-N′-(4-ethoxy-phenyl)methylidenebenzohydrazide Using a Multi-Spectroscopic Approach and Molecular Docking [O] . Tanveer A. Wani, Ahmed H. Bakheit, Abdul-Rahman A. Al-Majed, 2017

机译：牛血清白蛋白与新型抗炎药4-（13-二氧代-13-二氢-2H-异吲哚-2-基）-N-（4-乙氧基-苯基）的相互作用的研究亚甲基苯并肼的多光谱方法和分子对接
7. Synthesis and Biophysical Insights into the Binding of a Potent Anti-Proliferative Non-symmetric Bis-isatin Derivative with Bovine Serum Albumin: Spectroscopic and Molecular Docking Approaches [O] . Ali Saber Abdelhameed, Ahmed H. Bakheit, Mostafa S. Mohamed, 2017

机译：有效抗增殖非对称双靛红衍生物与牛血清白蛋白结合的合成和生物物理学见解：光谱和分子对接方法

Design and Synthesis of Novel 13-Thiazole and 2-Hydrazinyl-13-Thiazole Derivatives as Anti-Candida Agents: In Vitro Antifungal Screening Molecular Docking Study and Spectroscopic Investigation of their Binding Interaction with Bovine Serum Albumin

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