Synthesis and biological evaluation as AChE inhibitors of new indanones and thiaindanones related to donepezil
Synthesis and biological evaluation as AChE inhibitors of new indanones and thiaindanones related to donepezil
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DOI：
10.1016/j.ejmech.2005.07.009
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发表时间：
2005-12-01
影响因子：
6.7
通讯作者：
Rault, S
中科院分区：
文献类型：
--
作者：
Omran, Z;Cailly, T;Rault, S
合成了64个新的茚满酮和与多奈哌齐相关的硫茚满酮，并在体外评价其作为潜在的AChE抑制剂。其中，11个衍生物被发现抑制酶的亚微摩尔范围内，最好的化合物显示其抑制活性的IC 50在相同的范围（0.06 μ M）比参考化合物，多奈哌齐（IC 50 = 0.02 μ M）。(c)2005年，Elsevier SAS。All rights reserved.
Sixty-four new indanones, and thiaindanones related to donepezil were synthesized and evaluated in vitro as potential AChE inhibitors. Among them, 11 derivatives were found to inhibit the enzyme in the submicromolar range; the best compound revealed its inhibitory activity with an IC50 in the same range (0.06 mu M) than the reference compound, donepezil (IC50 = 0.02 mu M). (c) 2005 Elsevier SAS. All rights reserved.