To
aid the development of novel antibacterial agents that possess
a innovative mechanism of action, we built a series of novel dithiocarbamate-containing
4H-chromen-4-one derivatives. We evaluated the activities
of the derivatives against three plant pathogens Xanthomonas
oryzae pv oryzae (X. oryzae pv o.), Ralstonia solanacearum (R. solanacearum), and Xanthomonas axonopodis pv citri (X. axonopodis pv c.). The results of the antibacterial bioassay showed that
most of the target compounds displayed good inhibitory effects against X. oryzae pv o. and X. axonopodis pv c. Remarkably, compound E6 showed
the best in vitro antibacterial activity against X. axonopodis pv c., with an EC50 value of 0.11 μg/mL, which was better than those of thiodiazole
copper (59.97 μg/mL) and bismerthiazol (48.93 μg/mL).
Compound E14 exhibited the best in vitro antibacterial activity against X. oryzae pv o., with an EC50 value of 1.58 μg/mL, which
was better than those of thiodiazole copper (83.04 μg/mL) and
bismerthiazol (56.05 μg/mL). Scanning electron microscopy analysis
demonstrated that compounds E6 and E14 caused
the rupture or deformation of the cell membranes for X. axonopodis pv c. and X. oryzae pv o., respectively. In vivo antibacterial
activity test and the defensive enzymes activity test results indicated
that the compound E14 could reduce X. oryzae pv o. more effectively than thiodiazole-copper
or bismerthiazol.
Plant bacteria such
as Xanthomonas axonopodis
pv.
citri (Xac), Pseudomonas
syringae
pv. actinidiae (Psa), Xanthomonas oryzae
pv. oryzae (Xoo), and tobacco
mosaic virus (TMV) have created huge obstacles to the global trade
of food and economic crops. However, traditional chemical agents used
to control these plant diseases have gradually become disadvantageous
due to long-term irregular use. Therefore, finding new and efficient
antibacterial and antiviral agents is becoming imperative. In this
study, a series of myricetin derivatives containing a quinazolinone
moiety were designed and synthesized, and the antibacterial and antiviral
activities of these compounds were evaluated. The bioassay results
showed that some target compounds exhibited good antibacterial activities in vitro and antiviral activities in vivo. Among them, the median effective concentration (EC50) value of compound L18 against Xac was 16.9 μg/mL, which was better than those of the control
drugs bismerthiazol (BT) (62.2 μg/mL) and thiodiazole copper
(TC) (97.5 μg/mL). Scanning electron microscopy (SEM) results
confirmed that compound L18 inhibited the growth of Xac by affecting the morphology of cells. Microscale thermophoresis
(MST) test results indicated that the dissociation constant (K
d) value of compound L11 against
TMV-CP was 0.012 μM, which was better than that of the control
agent ningnanmycin (2.726 μM). This study reveals that myricetin
derivatives containing a quinazolinone moiety are potential antibacterial
and antiviral agents.
Various 1,3,4-oxadiazole thioether 4H-chromen-4-one derivatives were conceived. The title compounds demonstrated striking inhibitory effects against Xac, Psa, and Xoo. EC 50 data exhibited that A8 (19.7 μg/mL) had better antibacterial activity against Xoo than myricetin, BT, and TC. Simultaneously, the mechanism of action of A8 had been verified by SEM. The results of anti-tobacco mosaic virus indicated that A9 had the best in vivo antiviral effect compared with ningnanmycin. From the data of MST, it could be seen that A9 (0.003 ± 0.001 μmol/L) exhibited a strong binding capacity, which was far superior to ningnanmycin (2.726 ± 1.301 μmol/L). This study shows that the 1,3,4-oxadiazole thioether 4H-chromen-4-one derivatives may become agricultural drugs with great potential.
We present the design and implementation of the XSQ system for querying streaming XML data using XPath 1.0. Using a clean design based on a hierarchical arrangement of pushdown transducers augmented with buffers, XSQ supports features such as multiple predicates, closures, and aggregation. XSQ not only provides high throughput, but is also memory efficient: It buffers only data that must be buffered by any streaming XPath processor. We also present an empirical study of the performance characteristics of XPath features, as embodied by XSQ and several other systems. root@ 2. 9 pub@ 3. 9 book id="1"@ 4.
A series of novel chalcone malonate derivatives were synthesized and their antibacterial and antiviral activities were evaluated. All target compounds were characterized by spectral data. The results of antimicrobial bioassay showed that one compound (diethyl [3-(naphthalen-2-yl)-1-(3-nitrophenyl)-3-oxopropyl]propanedioate) showed excellent antibacterial activity against Xanthomonas oryzae pv. oryzae (Xoo), with an EC 50 value of 10.2 μg/mL, which is significantly superior to bismerthiazol (71.7 μg/mL) and thiodiazole copper (97.8 μg/mL). At the same time, the mechanism of two compounds was confirmed by scanning electron microscopy. In addition, another compound (diethyl [3-(naphthalen-2-yl)-1-(4-nitrophenyl)-3-oxopropyl]propanedioate) showed significant curative activity to tobacco mosaic virus, with a value of 74.3 %, which was superior to 53.3 % of ningnanmycin. The results of microscale thermophoresis also showed that the Kd value of the combination of two compounds with the coat protein of tobacco mosaic virus was 0.211 and 0.166 μmol/L, which was better than 0.596 μmol/L of ningnanmycin. At the same time, the molecular docking of two compounds with tobacco mosaic virus-coat protein shows that the compound is well embedded in the pocket between the two subunits of tobacco mosaic virus-coat protein. These results show that chalcone derivatives containing malonate group can be considered as activators in the design of antibacterial and antiviral agents.
A compact in-fiber integrated fiber-optic Michelson interferometer based accelerometer is proposed and investigated. In the system, the sensing element consists of a twin-core fiber acting as a bending simple supported beam. By demodulating the optical phase shift, we obtain that the acceleration is proportional to the force applied on the central position of the twin-core fiber. A simple model has been established to calculate the sensitivity and resonant frequency. The experimental results show that such an accelerometer has a sensitivity of 0.09 rad/g at the resonant frequency of 680 Hz.
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