- Synthesis and evaluation of caffeic acid amides as antioxidants
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A series of amides of caffeic acid has been synthesised and their antioxidant properties evaluated as lipid peroxidation inhibitors. Anilides of caffeic acid were found to be very efficient antioxidants with IC50's of 0.3 μM.
- Rajan, Padinchare,Vedernikova, Irina,Cos, Paul,Vanden Berghe, Dirk,Augustyns, Koen,Haemers, Achiel
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- Design, synthesis, and evaluation of caffeic acid amides as synergists to sensitize fluconazole-resistant Candida albicans to fluconazole
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A series of caffeic acid amides were designed, synthesized, and their synergistic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The title caffeic acid amides 3-30 except 26 exhibited potent activity, and the subsequent SAR study was conducted. Compound 3, 5, 21, and 34c, at a concentration of 1.0 μg/ml, decreased the MIC80 of fluconazole from 128.0 μg/ml to 1.0-0.5 μg/ml against the fluconazole-resistant C. albicans. This result suggests that the caffeic acid amides, as synergists, can sensitize drug-resistant fungi to fluconazole. The SAR study indicated that the dihydroxyl groups and the amido groups linking to phenyl or heterocyclic rings are the important pharmacophores of the caffeic acid amides.
- Dai, Li,Zang, Chengxu,Tian, Shujuan,Liu, Wei,Tan, Shanlun,Cai, Zhan,Ni, Tingjunhong,An, Maomao,Li, Ran,Gao, Yue,Zhang, Dazhi,Jiang, Yuanying
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- Design, synthesis and biological evaluation of caffeic acid amides as selective MMP-2 and MMP-9 inhibitors
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Strategy, Management and Health Policy Preclinical Research A series of caffeic acid amides with extended P1' groups were synthesized and tested for their inhibitory activities on matrix metalloproteinase (MMP)-1, MMP-2, and MMP-9. Compound 3f showed considerable inhibitory activities against MMP-2, MMP-9, and best selectivity over MMP-1. Preliminary structure-activity relationship analysis and docking studies indicated that caffeic acid amides with electron-donating groups at p-position of amino phenyl group showed better inhibitory activities and selectivity than those with electron-withdrawing groups. The findings of this study would provide information for the exploitation and utilization of caffeic acid as MMP inhibitor for metastatic tumor treatment.
- Shi, Zhi-Hao,Li, Nian-Guang,Shi, Qian-Ping,Tang, Hao,Tang, Yu-Ping,Li, Wei,Yin, Lian,Yang, Jian-Ping,Duan, Jin-Ao
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p. 343 - 351
(2012/10/29)
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- Evaluation of caffeic acid amide analogues as anti-platelet aggregation and anti-oxidative agents
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A series of amides of caffeic acid were synthesized and evaluated for their anti-platelet and anti-oxidative activities. N-(2-Bromo-phenyl)-3-(3,4- dihydroxy-phenyl)-acrylamide (12) and N-(3-Bromo-phenyl)-3-(3,4-dihydroxy- phenyl)-acrylamide (13) exhibite
- Hung, Chia-Cheng,Tsai, Wei-Jen,Kuo, Li-Ming Yang,Kuo, Yao-Haur
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p. 1791 - 1797
(2008/02/02)
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