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Identification of a diverse synthetic abietane diterpenoid library and insight into the structure-activity relationships for antibacterial activity |
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| Authors: | Wei Hou Guanjun Zhang Zhi Luo Di Li Haoqiang Ruan Benfang Helen Ruan Lin Su Hongtao Xu |
| Institution: | 1. College of Pharmaceutical Science, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China;2. College of Chemical Engineering and Materials Science, Tianjin University of Science & Technology, Tianjin 300457, PR China;3. Shanghai Evergene Biotech Co., Ltd., Shanghai 201499, PR China;4. Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, PR China |
| Abstract: | A diverse natural product-like (NPL) synthetic abietane diterpenoid library containing 86 compounds were obtained and the SARs were studied based on their antibacterial potential. Further in vitro cytotoxic and in silico drug-like properties evaluation showed that the potent antibacterial compound 84 had good drug-like properties and displayed low cytotoxicity toward noncancerous mammalian cells, indicating the study of AA and DHAA might be a good starting point for the search of novel antimicrobial molecules. Future work should be focused on the optimization of their potency and selectivity. |
| Keywords: | Diterpenoid Natural product-like (NPL) Dehydroabietic acid (DHAA) Abietic acid (AA) Click chemistry Antibacterial |
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