Synthesis, Antibacterial and Pharmacokinetic Evaluation of Novel Derivatives of Harmine N9-Cinnamic Acid

A series of 16 new derivatives of harmine N9-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 (S. aureus, S....

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2021-08, Vol.26 (16), p.4842
Main Authors: Liang, Yan, He, Dian, Zhou, Deshun, Li, Junshuai, Tang, Lei, Wang, Zhen
Format: Article
Language:English
Subjects:
Acids
Antibacterial activity
Antibiotics
Bactericidal activity
Bioavailability
Biocompatibility
Cell lines
Chromatography
Cinnamic acid
Cytotoxicity
Drug resistance
E coli
harmine
In vivo methods and tests
Minimum inhibitory concentration
NMR
Nuclear magnetic resonance
Pharmacokinetics
Pharmacology
Plasma
Reagents
Solvents
Staphylococcus infections
synthesis
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Summary:A series of 16 new derivatives of harmine N9-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 (S. aureus, S. albus and MRSA) than Gram-negative strains (E. coli and PA). In particular, compound 3c showed the strongest bactericidal activity with a minimum inhibitory concentration of 13.67 μg/mL. MTT assay showed that compound 3c displayed weaker cytotoxicity than harmine with IC50 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 3c in vivo were rapid in rats with an oral bioavailability of 6.9%.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules26164842