期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 7, 页码 1766-1770出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.02.031
关键词
Antidepressant; Benzoxazole/benzothiazole; 2,3-Dihydrobenzo[b][1,4]dioxine; 5-HT1A; 5-HT2A
资金
- Jiangsu Nhwa Pharmaceutical
- Huazhong University of Science and Technology Analytical and Testing Center
A series of benzoxazole/benzothiazole-2,3-dihydrobenzo[b][ 1,4] dioxine derivatives (5a-5d and 8a-8j) was synthesized. Compounds were evaluated for binding affinities at the 5-HT1A and 5-HT2A receptors. Antidepressant activities of the compounds were screened using the forced swimming test (FST) and the tail suspension test (TST). The results indicated that the compounds exhibited high affinities for the 5-HT1A and 5-HT2A receptors and showed a marked antidepressant-like activity. Compound 8g exhibited high affinities for the 5-HT1A (K-i = 17 nM) and 5-HT2A (K-i = 0.71 nM) receptors; it also produced a decrease of the immobility time and exhibited potent antidepressant-like effects in the FST and TST in mice. (C) 2014 Elsevier Ltd. All rights reserved.
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