Design, synthesis and biological evaluation of soluble 2,5-diketopiperazines derivatives as potential antifouling agents
Liao, Shengrong1; Xu, Ying1; Tang, Yong1; Wang, Junfeng1; Zhou, Xuefeng1; Xu, Liang1; Liu, Yonghong1; ljrss@126.com; boxuying@szu.edu.cn; 307091847@qq.com; junfeng1982a@163.com; xfzhou@scsio.ac.cn; xuliang@enantiotech.net; yonghongliu@scsio.ac.cn
2015
发表期刊RSC ADVANCES
卷号5期号:63页码:51020-51026
摘要A small library of soluble 2,5-diketopiperazine derivatives were designed, synthesized and evaluated as antifouling agents against two species of marine organisms: Balanus amphitrite and Bugula neritina by larval attachment assay. The results showed that different derivatives had different antifouling activities. Among these compounds, 3a (EC50 = 2.5 mu g mL(-1)), 3b (EC50 = 3.2 mg mL(-1)) and 3d (EC50 = 1.6 mg mL(-1)) had strong activities, and 2d (EC50 = 20.5 mg mL(-1)), 3l (EC50 = 25.0 mg mL(-1)) and 3m (EC50 = 18.5 mg mL(-1)) had moderate activities against Balanus amphitrite, but other compounds had no activities. Differently, compounds 3d (EC50 = 3.1 mg mL(-1)) and 3i (EC50 = 2.3 mg mL(-1)) exhibited strong activities, and 3a (EC50 = 11.3 mg mL(-1)) and 3c (EC50 = 17.2 mg mL(-1)) showed moderate activities against Bugula neritina, whereas other compounds had no activities. All of the active compounds had stronger antifouling activities than those of the natural product cyclo-(L-Phe-L-Pro). Compound 3d could be a new template molecule for further development as an antifouling agent because of its strong inhibitory activities against both species of fouling organisms with low or no toxicity to the environment.
部门归属LMB
学科领域Chemistry
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文献类型期刊论文
条目标识符http://ir.scsio.ac.cn/handle/344004/14891
专题中科院海洋生物资源可持续利用重点实验室
通讯作者ljrss@126.com; boxuying@szu.edu.cn; 307091847@qq.com; junfeng1982a@163.com; xfzhou@scsio.ac.cn; xuliang@enantiotech.net; yonghongliu@scsio.ac.cn
作者单位1.[Liao, Shengrong
2.Tang, Yong
3.Wang, Junfeng
4.Zhou, Xuefeng
5.Liu, Yonghong] Chinese Acad Sci, South China Sea Inst Oceanol, CAS Key Lab Trop Marine Bioresources & Ecol, Guangdong Key Lab Marine Mat Med,Res Ctr Marine M, Guangzhou 510301, Guangdong, Peoples R China
6.[Xu, Ying] Shenzhen Univ, Coll Life Sci, Shenzhen Engn Lab Marine Algal Biotechnol, Shenzhen Key Lab Marine Bioresource & Ecoenvironm, Shenzhen 518060, Peoples R China
7.[Xu, Liang] Enantiotech Corp Ltd, Zhongshan Torch Hitech, Zhongshan 528437, Peoples R China
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Liao, Shengrong,Xu, Ying,Tang, Yong,et al. Design, synthesis and biological evaluation of soluble 2,5-diketopiperazines derivatives as potential antifouling agents[J]. RSC ADVANCES,2015,5(63):51020-51026.
APA Liao, Shengrong.,Xu, Ying.,Tang, Yong.,Wang, Junfeng.,Zhou, Xuefeng.,...&yonghongliu@scsio.ac.cn.(2015).Design, synthesis and biological evaluation of soluble 2,5-diketopiperazines derivatives as potential antifouling agents.RSC ADVANCES,5(63),51020-51026.
MLA Liao, Shengrong,et al."Design, synthesis and biological evaluation of soluble 2,5-diketopiperazines derivatives as potential antifouling agents".RSC ADVANCES 5.63(2015):51020-51026.
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