A series of eleven ethoxysubstituted chalcones (E1-E11) were synthesized and investigated for their inhibitory potential towards human recombinant monoamine oxidase A and B (hMAOÀ A and hMAOÀ B, respectively) and acetylcholinesterase (AChE). IC 50 values of 4.63 � 0.15 and 0.053 � 0.003 μM were obtained for MAOÀ A and MAOÀ B, respectively, by the most interesting compound (2E)-1-(4-ethoxyphenyl)-3-(4-fluorophenyl)prop-2-en-1-one (E7), and it was characterized by a high selectivity index (SI = 87.4) for MAOÀ B. Inhibitions by E7 against MAOÀ A and MAOÀ B were recovered (75.9 and 74.5%, respectively) to near the levels of reversible references (77.1 and 77.4%, respectively). The inhibition modes of E7 for MAOÀ A and MAOÀ B were competitive with K i values of 2.65 � 0.064 and 0.011 � 0.0011 μM, respectively. Compounds (2E)-1-(4ethoxyphenyl)-3-(4-ethylphenyl) prop-2-en-1-one (E10) and (2E)-1-(4-ethoxyphenyl)-3-[4-(trifluoromethyl)phenyl]prop-2-en-1-one (E11) showed good inhibitions against AChE with IC 50 values of 2.86 � 0.041 and 3.23 � 0.0073 μM, respectively. A combined molecular docking/MM-GBSA approach was used that employed quantum mechanics (QM) partial charges; this technique revealed the molecular rationale behind the observed MAOÀ B selectivity for this molecular series. Taken together, these results indicate that E7 is a potent, selective and reversible competitive inhibitor of MAOÀ B with moderately potent AChE inhibitory activity that has potential as a multitargeting drug
The title compounds were synthesized by condensation of 3-acetyl chromen-2-one with benzaldehyde in presence of alcoholic sodium hydroxide to get intermediate 3-(3-phenyl acryloyl) chromen-2-one, which were further treated with hydrazine hydrate to get 3-(5-phenyl-4,5-dihydro-1H-pyrazol-3-yl) chromen-2-one. The latter were refluxed with various amino compounds and various aldehyde derivatives on water bath for 5 h to afford title compounds. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.
Some new 3-(substituted)-chromen-2-one have been synthesized by condensation of 3-acetylchromen-2-one with various aromatic aldehyde in presence of ethanol and alkali. The synthesized compounds were identified by spectral data and screened for their antibacterial activity againstB. pumilis, B. substilisandE. coliand antifungal activity againstA. nigerandCandida albicans. Among the synthesized compounds, some compounds of aryl chromen, which are having electron releasing substituent such as methoxy and hydroxyl at various positions, showed moderate to considerable antibacterial and antifungal activities.
Automatic Target Recognition (ATR) is the process of aided or unaided target detection and recognitionusing data from different sensors. Fusion techniques are used to improve ATR since this reduces system dependence on a single sensor and increases noise tolerance. In this work, ATR is performed on civilian targets which are considered more difficult to classify than military targets. The dataset is provided by the Night Vision & Electronic Sensors Directorate (NVESD) and is collected using the Sensor Fusion TestBed (SFTB) developed by Northrop Grumman Mission Systems. Stationary color and infrared cameras capture images of seven different vehicles at different orientations and distances. Targets include two sedans, two SUVs, two light trucks and a heavy truck. Fusion is performed at the event level and sensor level using temporal and Behavior-Knowledge-Space (BKS) fusion respectively. It is shown that fusion provides better and robust classification compared to classification of individual frames without fusion. The classification experiment shows, on an average, mean classification rates of 65.0%, 70.1% and 77.7% for individual frame classification, temporal fusion and BKS fusion respectively. It is demonstrated that the classification accuracy increases as the level of fusion goes higher. By combining targets into cars, SUVs and light trucks and thereby reducing the number of classes to three, higher mean classification rates of 75.4%, 90.0% and 94.8% were obtained.
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