42381-67-9Relevant academic research and scientific papers
Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents
Fang, Lei,Chen, Mohao,Liu, Zhikun,Fang, Xubin,Gou, Shaohua,Chen, Li
, p. 886 - 893 (2016/02/09)
In order to search for novel multifunctional anti-Alzheimer agents, a series of ferulic acid-carbazole hybrid compounds were designed and synthesized. Ellman's assay revealed that the hybrid compounds showed moderate to potent inhibitory activity against the cholinesterases. Particularly, the AChE inhibition potency of compound 5k (IC50 1.9 μM) was even 5-fold higher than that of galantamine. In addition, the target compounds showed pronounced antioxidant ability and neuroprotective property, especially against the ROS-induced toxicity. Notably, the neuroprotective effect of 5k was obviously superior to that of the mixture of ferulic acid and carbazole, indicating the therapeutic effect of the hybrid compound is better than the combination administration of the corresponding mixture.
Biological activity evaluation and structure-activity relationships analysis of ferulic acid and caffeic acid derivatives for anticancer
Li, Weixia,Li, Nianguang,Tang, Yuping,Li, Baoquan,Liu, Li,Zhang, Xu,Fu, Haian,Duan, Jin-Ao
, p. 6085 - 6088 (2012/10/29)
The anticancer activities of alkyl esters and NO-donors of ferulic acid (FA) and caffeic acid (CA) were assessed by a high-throughout screening (HTS) method, and the structure-activity relationships were described. CA alkyl esters had better anticancer activities than FA alkyl esters with the same alkyl substituent. Mono-nitrates and phenylfuroxan nitrates were more potent than the dual nitrates. Phenylsulfonylfuroxan nitrates of FA, especially compounds 8b-8d, exhibited more potent activities in anticancer.
Design and synthesis of novel NO-donor-ferulic acid hybrids as potential antiatherosclerotic drug candidates a
Li, Nian-Guang,Wang, Rong,Shi, Zhi-Hao,Tang, Yu-Ping,Li, Bao-Quan,Wang, Zhen-Jiang,Song, Shu-Lin,Qian, Li-Hua,Wei, Li,Yang, Jian-Ping,Yao, Li-Juan,Xi, Jun-Zuan,Xu, Jia,Feng, Feng,Qian, Da-Wei,Duan, Jin-Ao
experimental part, p. 405 - 415 (2012/05/05)
Novel NO-donor-ferulic acid hybrids were designed and synthesized through a symbiotic approach using ferulic acid and three different NO-donating groups, such as nitric ester, 4-hydroxyl-3-phenylfuroxan, and 4-hydroxymethyl-3- phenylsulfonylfuroxan. Antioxidant, nitric oxide release, and vasodilator properties studies showed that the target phenylsulfonylfuroxan 14, especially 14c, while keeping the antioxidant activity, showed more NO release activity and vasodilating activity than isosorbide dinitrate (ISDN). Thus, 14c may be considered a novel potent anti-atherosclerosis drug candidate.
Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates
Fang, Lei,Kraus, Birgit,Lehmann, Jochen,Heilmann, Joerg,Zhang, Yihua,Decker, Michael
, p. 2905 - 2909 (2008/12/22)
Five tacrine-ferulic acid hybrids (6a-e) were designed and synthesized as multi-potent anti-Alzheimer drug candidates. All target compounds have better acetylcholinesterase inhibitory activity and comparable butyrylcholinesterase inhibitory activity in relation to tacrine. Interestingly, 6d showed a reversible and non-competitive inhibitory action for acetylcholinesterase indicating interaction with the peripheral anionic site, whereas a reversible but competitive inhibitory action for butyrylcholinesterase. The antioxidant study revealed that four target compounds have, compared to Trolox, high ability to absorb reactive oxygen species.
