Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.

Singh K; Wan B; Franzblau S; Chibale K; Balzarini J

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Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.

机译：从Biginelli嘧啶2（1H）-一到嘧啶的简便转化。作为结核分枝杆菌抑制剂和细胞抑制活性调节剂的体外评估。

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A series of pyrimidine derivatives bearing amine substituents at C-2 position were obtained from Biginelli 3,4-dihydropyrimidin-2(1H)-ones and the effect of structural variation on anti-TB activity against Mycobacterium tuberculosis H37Rv strain and antiviral activity in a series of cell cultures was evaluated. While the compounds were found to possess structure dependent cytostatic activity, these were not found to be efficient inhibitors of M. tuberculosis nor did they inhibit a broad variety of DNA or RNA viruses in cell culture.

机译：从Biginelli 3,4-dihydropyrimidin-2（1H）-ones获得了一系列在C-2位置带有胺取代基的嘧啶衍生物，以及结构变异对结核分枝杆菌H37Rv菌株抗TB活性和抗病毒活性的影响。评估了一系列细胞培养。尽管发现这些化合物具有结构依赖性的细胞抑制活性，但这些化合物不是结核分枝杆菌的有效抑制剂，也不能抑制细胞培养物中的多种DNA或RNA病毒。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2011年第6期|共5页
作者
Singh K; Wan B; Franzblau S; Chibale K; Balzarini J;
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1. Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity. [J] . Singh K, Wan B, Franzblau S, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2011,第6期

机译：从Biginelli嘧啶2（1H）-一到嘧啶的简便转化。作为结核分枝杆菌抑制剂和细胞抑制活性调节剂的体外评估。
2. Evaluation of the in vitro antiretroviral potential of some Biginelli-type pyrimidines. [J] . R Zabihollahi, R Vahabpour, C Hartoonian, Acta Virologica: International Journal . 2012,第1期

机译：评估一些Biginelli型嘧啶的体外抗逆转录病毒潜力。
3. Regioselective synthesis of novel 4,5-diaryl functionalized 3,4-dihydropyrimidine-2(1H)-thiones via a non-Biginelli-type approach and evaluation of their in vitro anticancer activity [J] . Jacek G. Sosnicki, Lukasz Struk, Mateusz Kurzawski, Organic & biomolecular chemistry . 2014,第21期

机译：通过非Biginelli型方法区域选择性合成新型4,5-二芳基官能化3,4-二氢嘧啶-2（1H）-硫酮并评估其体外抗癌活性
4. Design synthesis and in vitro biological evaluation of novel benzimidazole tethered allylidenehydrazinylmethylthiazole derivatives as potent inhibitors of Mycobacterium tuberculosis [O] . Goverdhan Surineni, Yamin Gao, Muzammal Hussain, 2019

机译：设计合成和体外生物学评价新型苯并咪唑系链的烯丙基亚水肼基甲基噻唑衍生物作为结核分枝杆菌的有效抑制剂
5. Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity [O] . Singh Kamaljit, Singh Kawaljit, Wan Baojie, 2011

机译：从Biginelli嘧啶2（1H）-一到嘧啶的简便转化。体外评估作为结核分枝杆菌抑制剂和细胞抑制活性调节剂

Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.

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