Narwal Sangeeta, Kumar Sanjiv, Verma Prabhakar Kumar
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, 124001, India.
Chem Cent J. 2017 Jun 9;11(1):52. doi: 10.1186/s13065-017-0284-2.
Pyrimidine is an aromatic heterocyclic moiety containing nitrogen atom at 1st and 3rd positions and play an important role to forms the central core for different necessity of biological active compounds, from this facts, we have designed and synthesized a new class of pyrimidin-2-ol/thiol/amine derivatives and screened for its in vitro antimicrobial activity.
The synthesized pyrimidine derivatives were confirmed by IR, H/C-NMR, Mass spectral studies and evaluated for their in vitro antimicrobial potential against Gram positive (S. aureus and B. subtilis), Gram negative (E. coli, P. aeruginosa and S. enterica) bacterial strains and fungal strain (C. albicans and A. niger) by tube dilution method and recorded minimum inhibitory concentration in µM/ml. The MBC and MFC values represent the lowest concentration of compound that produces in the range of 96-98% end point reduction of the used test bacterial and fungal species.
In general all synthesized derivatives exhibited good antimicrobial activity. Among them, compounds 2, 5, 10, 11 and 12 have significant antimicrobial activity against used bacterial and fungal strains and also found to be more active than the standard drugs. Graphical abstract Pyrimidine is an aromatic heterocyclic moiety containing nitrogen atom at 1st and 3rd positions and play an important role to forms the central core for different necessity of biological active compounds, from this facts, we have designed and synthesized a new class of pyrimidin-2-ol/thiol/amine derivatives and screened for its in vitro antimicrobial activity. The synthesized pyrimidine derivatives were confirmed by IR, 1H/13C-NMR, Mass spectral studies and evaluated for their in vitro antimicrobial potential against Gram positive (S. aureus and B. subtilis), Gram negative (E. coli, P. aeruginosa and S. enterica) bacterial strains and fungal strain (C. albicans and A. niger) by tube dilution method and recorded minimum inhibitory concentration in µM/ml. The MBC and MFC values represent the lowest concentration of compound that produces in the range of 96-98% end point reduction of the used test bacterial and fungal species.
嘧啶是一种在第1和第3位含有氮原子的芳香杂环部分，对于形成不同生物活性化合物所需的核心结构起着重要作用。基于此，我们设计并合成了一类新型的嘧啶-2-醇/硫醇/胺衍生物，并对其体外抗菌活性进行了筛选。
通过红外光谱（IR）、氢/碳核磁共振（H/C-NMR）、质谱研究对合成的嘧啶衍生物进行了确证，并采用试管稀释法评估了它们对革兰氏阳性菌（金黄色葡萄球菌和枯草芽孢杆菌）、革兰氏阴性菌（大肠杆菌、铜绿假单胞菌和肠炎沙门氏菌）以及真菌菌株（白色念珠菌和黑曲霉）的体外抗菌潜力，并记录了以微摩尔/毫升为单位的最低抑菌浓度。最低杀菌浓度（MBC）和最低真菌杀菌浓度（MFC）值代表了能使所用测试细菌和真菌物种的终点减少96 - 98%的化合物的最低浓度。
总体而言，所有合成衍生物均表现出良好的抗菌活性。其中，化合物2、5、10、11和12对所用细菌和真菌菌株具有显著的抗菌活性，并且发现其活性比标准药物更高。图形摘要嘧啶是一种在第1和第3位含有氮原子的芳香杂环部分，对于形成不同生物活性化合物所需的核心结构起着重要作用。基于此，我们设计并合成了一类新型的嘧啶-2-醇/硫醇/胺衍生物，并对其体外抗菌活性进行了筛选。通过红外光谱（IR）、氢/碳核磁共振（1H/13C-NMR）、质谱研究对合成的嘧啶衍生物进行了确证，并采用试管稀释法评估了它们对革兰氏阳性菌（金黄色葡萄球菌和枯草芽孢杆菌）、革兰氏阴性菌（大肠杆菌、铜绿假单胞菌和肠炎沙门氏菌）以及真菌菌株（白色念珠菌和黑曲霉）的体外抗菌潜力，并记录了以微摩尔/毫升为单位的最低抑菌浓度。最低杀菌浓度（MBC）和最低真菌杀菌浓度（MFC）值代表了能使所用测试细菌和真菌物种的终点减少96 - 98%的化合物的最低浓度。
