Novel 5H-[1,2,4]oxadiazolo[4,5-a]pyrimidin-5-one derivatives as antibacterial and anticancer agents: Synthesis and biological evaluation |
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Authors: | Xiaoyu Liu Xizhong Song Yuwen Liu Mingjin Xie Wei Yu Shengjiao Yan Jun Lin Yi Jin |
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Institution: | 1. Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China;2. Pharmaceutical Department, Kunming General Hospital of Chengdu Military Command, Kunming 650118, PR China;3. Jiangxi Qing Chun Kang Yuan Pharmaceutical Co., Ltd., Xinyu 336600, PR China |
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Abstract: | A novel class of 5H-1,2,4]oxadiazolo4,5-a]pyrimidine derivatives was prepared, characterized, and tested for its antibacterial and anticancer potential against thirteen strains and five human cancer cell lines. The synthetic method was optimized, and a proposed reaction mechanism was also presented. The compounds containing the 5-bromo-pyrimidine moiety exhibited moderate antibacterial potencies against Gram-positive strains. Furthermore, the newly prepared compounds displayed selectively antiproliferative activity against human cancer cell lines. These current results will help us to further optimize and develop new drug candidates for clinical studies as novel antibacterial or anticancer agents. |
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Keywords: | Oxadiazole Pyrimidine Antibacterial activity Anticancer activity |
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