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 identified as potent and safe antidepressant lead compounds.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China.
Shuyi
S
Yao
Hui
H
Xie
Li
L
Zhang
Tao
T
Meng
Yongliang
Y
Zhang
Xin
X
Wang
Lin
L
Chen
Shengli
S
Pan
Jingkang
J
Shen
D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D052117:Benzodioxoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
D000928:Antidepressive Agents; D052117:Benzodioxoles; C512035:N-isobutyl-(3,4-methylenedioxyphenyl)-2,4,9-undecatrienoamide