Total synthesis and antidepressant activities of laetispicine and its derivatives

The first total synthesis of laetispicine (1a), an amide alkaloid isolated from the stems of Piper laetispicum C.DC (Piperaceae), and the synthesis of some of its derivatives were described. Based on the evaluation of antidepressant activities in the forced swimming test, compounds 1h and 1i were id...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2012-02, Vol.17 (2), p.1425-1436
Main Authors: Yao, Shuyi, Xie, Hui, Zhang, Li, Meng, Tao, Zhang, Yongliang, Wang, Xin, Chen, Lin, Pan, Shengli, Shen, Jingkang
Format: Article
Language:English
Subjects:
antidepressant
Antidepressants
Antidepressive Agents - chemical synthesis
Antidepressive Agents - pharmacology
Benzodioxoles - chemical synthesis
Benzodioxoles - pharmacology
Drug Evaluation, Preclinical
forced swimming test
laetispicine derivatives
Magnetic Resonance Spectroscopy
Natural products
Potassium
Reagents
Spectrometry, Mass, Electrospray Ionization
total synthesis
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Summary:The first total synthesis of laetispicine (1a), an amide alkaloid isolated from the stems of Piper laetispicum C.DC (Piperaceae), and the synthesis of some of its derivatives were described. Based on the evaluation of antidepressant activities in the forced swimming test, compounds 1h and 1i were identified as potent and safe antidepressant lead compounds.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules17021425