| Summary: | A series of 16 new derivatives of harmine N<sup>9</sup>-Cinnamic acid were synthesized and fully characterized using NMR and MS. The in vitro antibacterial evaluation revealed that most of the synthesized harmine derivatives displayed better antibacterial activities against Gram-positive strains (<i>S. aureus</i>, <i>S. albus</i> and MRSA) than Gram-negative strains (<i>E. coli</i> and PA). In particular, compound <b>3c</b> showed the strongest bactericidal activity with a minimum inhibitory concentration of 13.67 μg/mL. MTT assay showed that compound <b>3c</b> displayed weaker cytotoxicity than harmine with IC<sub>50</sub> of 340.30, 94.86 and 161.67 μmol/L against WI-38, MCF-7 and HepG2 cell lines, respectively. The pharmacokinetic study revealed that the distribution and elimination of <b>3c</b> in vivo were rapid in rats with an oral bioavailability of 6.9%.
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