基于点击反应的新型1,2,3-三唑的合成、抗菌及细胞毒性活性
Click reaction based synthesis, antimicrobial, and cytotoxic activities of new 1,2,3-triazoles.
作者信息
El Sayed Aly Mohamed Ramadan, Saad Hosam Ali, Mohamed Mosselhi Abdelnabi Mosselhi
机构信息
Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Applied Science, Port Said University, 42522 Port Said, Egypt.
Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Science, Zagazig University, Zagazig 44511, Egypt.
出版信息
Bioorg Med Chem Lett. 2015 Jul 15;25(14):2824-30. doi: 10.1016/j.bmcl.2015.04.096. Epub 2015 May 6.
Three-motif pharmacophoric models 20a-e and 21-25 were prepared in good yields by CuAAC of two azido substrates 2 and 11 with seven terminal acetylenic derivatives including chalcones 17a-e, theophylline 18 and cholesterol 19. The structure of these compounds was elucidated by NMR, MS, IR spectroscopy and micro analyses. This series was screened as antimicrobial and cytotoxic agents in vitro. Most derivatives showed appreciable antibacterial activity, but they displayed weak cytotoxic, and antifungal activities. Notably, conjugate 25 (cream of the crop) was found to be more active than Ampicillin against Escherichia coli and Staphylococcus aureus and showed appreciable antifungal and cytotoxic activities as well.
通过两个叠氮基底物2和11与七种末端炔衍生物（包括查耳酮17a - e、茶碱18和胆固醇19）的铜催化的叠氮-炔环加成反应（CuAAC），以良好的产率制备了三基序药效团模型20a - e和21 - 25。通过核磁共振（NMR）、质谱（MS）、红外光谱（IR）和微量分析对这些化合物的结构进行了阐明。对该系列化合物进行了体外抗菌和细胞毒性筛选。大多数衍生物表现出可观的抗菌活性，但它们的细胞毒性和抗真菌活性较弱。值得注意的是，共轭物25（佼佼者）对大肠杆菌和金黄色葡萄球菌的活性比氨苄青霉素更高，并且还表现出可观的抗真菌和细胞毒性活性。
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