Synthesis and Antibacterial Evaluation of N -phenylacetamide Derivatives Containing 4-arylthiazole Moieties
A series of new -phenylacetamide derivatives containing 4-arylthiazole moieties was designed and synthesized by introducing the thiazole moiety into the amide scaffold. The structures of the target compounds were confirmed by H-NMR, C-NMR and HRMS. Their in vitro antibacterial activities were evalua...
Gespeichert in:
Veröffentlicht in: | Molecules (Basel, Switzerland) Switzerland), 2020-04, Vol.25 (8), p.1772 |
---|---|
Hauptverfasser: | , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | A series of new
-phenylacetamide derivatives containing 4-arylthiazole moieties was designed and synthesized by introducing the thiazole moiety into the amide scaffold. The structures of the target compounds were confirmed by
H-NMR,
C-NMR and HRMS. Their in vitro antibacterial activities were evaluated against three kinds of bacteria-
pv.
(
),
pv.
(
) and
pv
(
)-showing promising results. The minimum 50% effective concentration (EC
) value of
(4-((4-(4-fluoro-phenyl)thiazol-2-yl)amino)phenyl)acetamide (
) is 156.7 µM, which is superior to bismerthiazol (230.5 µM) and thiodiazole copper (545.2 µM). A scanning electron microscopy (SEM) investigation has confirmed that compound
could cause cell membrane rupture of
. In addition, the nematicidal activity of the compounds against
(
) was also tested, and compound
displayed excellent nematicidal activity, with mortality of 100% and 53.2% at 500 μg/mL and 100 μg/mL after 24 h of treatment, respectively. The preliminary structure-activity relationship (SAR) studies of these compounds are also briefly described. These results demonstrated that phenylacetamide derivatives may be considered as potential leads in the design of antibacterial agents. |
---|---|
ISSN: | 1420-3049 1420-3049 |
DOI: | 10.3390/molecules25081772 |