2 research outputs found
Synthesis, Antibacterial Activity, and Mechanisms of Novel Indole Derivatives Containing Pyridinium Moieties
The development of effective antibacterial agents equipped
with
novel action modes and unique skeletons starting from natural compounds
serves as an important strategy in the modern pesticide industry.
Disclosed here are a series of novel indole derivatives containing
pyridinium moieties and their antibacterial activity evaluation against
two prevalent phytopathogenic bacteria, Xanthomonas
oryzae pv. oryzicola (Xoc) and X. oryzae pv. oryzae (Xoo). A three-dimensional (3D)-QSAR model was
adopted to discover higher activity like title compounds based on
the Xoc antibacterial activity of the tested compounds.
Compound 43 was consequently designed, and it displayed
higher antibacterial activity as expected with the half-maximal effective
concentration EC50 values of 1.0 and 1.9 μg/mL for Xoo and Xoc, respectively, which were better
than those of the commercial drug thiodiazole copper (TC) (72.9 and
87.5 μg/mL). Under greenhouse conditions, the results of a rice in vivo pot experiment indicated that the protective and
curative activities of compound 43 against rice bacterial
leaf streak (BLS) and rice bacterial blight (BLB) were 45.0 and 44.0%
and 42.0 and 39.3%, respectively, which were better than those of
the commercial agent thiodiazole copper (38.0 and 37.9%, 38.6 and
37.0%) as well. Scanning electron microscopy images, defense enzyme
activity tests, and proteomic techniques were utilized in a preliminary
mechanism study, suggesting that compound 43 shall modulate
and interfere with the physiological processes and functions of pathogenic
bacteria
Synthesis, Antibacterial Activity, and Mechanisms of Novel Indole Derivatives Containing Pyridinium Moieties
The development of effective antibacterial agents equipped
with
novel action modes and unique skeletons starting from natural compounds
serves as an important strategy in the modern pesticide industry.
Disclosed here are a series of novel indole derivatives containing
pyridinium moieties and their antibacterial activity evaluation against
two prevalent phytopathogenic bacteria, Xanthomonas
oryzae pv. oryzicola (Xoc) and X. oryzae pv. oryzae (Xoo). A three-dimensional (3D)-QSAR model was
adopted to discover higher activity like title compounds based on
the Xoc antibacterial activity of the tested compounds.
Compound 43 was consequently designed, and it displayed
higher antibacterial activity as expected with the half-maximal effective
concentration EC50 values of 1.0 and 1.9 μg/mL for Xoo and Xoc, respectively, which were better
than those of the commercial drug thiodiazole copper (TC) (72.9 and
87.5 μg/mL). Under greenhouse conditions, the results of a rice in vivo pot experiment indicated that the protective and
curative activities of compound 43 against rice bacterial
leaf streak (BLS) and rice bacterial blight (BLB) were 45.0 and 44.0%
and 42.0 and 39.3%, respectively, which were better than those of
the commercial agent thiodiazole copper (38.0 and 37.9%, 38.6 and
37.0%) as well. Scanning electron microscopy images, defense enzyme
activity tests, and proteomic techniques were utilized in a preliminary
mechanism study, suggesting that compound 43 shall modulate
and interfere with the physiological processes and functions of pathogenic
bacteria