Abstract:
: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 (Ki=17 nM) and 5-HT2A (Ki=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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Wang S,Chen Y,Zhao S,Xu X,Liu X,Liu BF,Zhang Gdoi
10.1016/j.bmcl.2014.02.031subject
Has Abstractpub_date
2014-04-01 00:00:00pages
1766-70issue
7eissn
0960-894Xissn
1464-3405pii
S0960-894X(14)00163-2journal_volume
24pub_type
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