Drone detection is a significant research topic due to the potential security threats posed by the misuse of drones in both civilian and military domains. However, traditional drone detection methods ...are challenged by the drastic scale changes and complex ambiguity during drone flight, and it is difficult to detect small target drones quickly and efficiently. We propose an information-enhanced model based on improved YOLOv5 (TGC-YOLOv5) for fast and accurate detection of small target drones in complex environments. The main contributions of this paper are as follows: First, the Transformer encoder module is incorporated into YOLOv5 to augment attention toward the regions of interest. Second, the Global Attention Mechanism (GAM) is embraced to mitigate information diffusion among distinct layers and amplify the global cross-dimensional interaction features. Finally, the Coordinate Attention Mechanism (CA) is incorporated into the bottleneck part of C3, enhancing the extraction capability of local information for small targets. To enhance and verify the robustness and generalization of the model, a small target drone dataset (SUAV-DATA) is constructed in all-weather, multi-scenario, and complex environments. The experimental results show that based on the SUAV-DATA dataset, the AP value of TGC-YOLOv5 reaches 0.848, which is 2.5% higher than the original YOLOv5, and the Recall value of TGC-YOLOv5 reaches 0.823, which is a 3.8% improvement over the original YOLOv5. The robustness of our proposed model is also verified on the Real-World open-source image dataset, achieving the best accuracy in light, fog, stain, and saturation pollution images. The findings and methods of this paper have important significance and value for improving the efficiency and precision of drone detection.
In continuation of our program to discover new potential pesticidal agents, thirty-one piperine analogs containing isoxazoline/pyrazoline scaffold were prepared, and confirmed by infrared spectra, ...proton/carbon-13 nuclear magnetic resonance spectra, and high-resolution mass spectra. The structures of compounds VIIb and VIIIc were further determined by 1H–1H COSY spectra. Especially the configuration of compound VIIIc was unambiguously confirmed by single-crystal X-ray diffraction. Their pesticidal activities were evaluated against three serious and typically crop-threatening agricultural pests, Tetranychus cinnabarinus Boisduval (spider mite), Mythimna separata Walker (Oriental armyworm), and Plutella xylostella Linnaeus (diamondback moth). Compounds VIIIb and VIIIc exhibited greater than 40-fold more potent acaricidal activity than the lead compound piperine against T. cinnabarinus. Notably, compounds VIa–c exhibited more pronounced oral toxicity against P. xylostella than toosendanin; compounds VIb and VIc displayed more promising growth inhibitory activity against M. separata than toosendanin. It demonstrated that the methylenedioxy and isoxazoline scaffolds were important for the oral toxicity and growth inhibitory activity against P. xylostella and M. separata, respectively; the ethylenedioxy and isoxazoline scaffolds were vital for the acaricidal activity against T. cinnabarinus. Moreover, compounds VIb, VIIf, and VIIIc showed very low toxicity against NRK-52E cells.
Infections caused by methicillin-resistant Staphylococcus aureus (MRSA) continue to endanger public health. Here, we report the synthesis of neolignan isomagnolone (I) and its isomer II, and the ...preparation of a series of novel neolignan-antimicrobial peptide (AMP) mimic conjugates. Notably, conjugates III5 and III15 exhibit potent anti-MRSA activity in vitro and in vivo, comparable to that of vancomycin, a current effective treatment for MRSA. Moreover, III5 and III15 display not only fast-killing kinetics and low resistance frequency but also low toxicity as well as effects on bacterial biofilms. Mechanism studies reveal that III5 and III15 exhibit rapid bactericidal effects through binding to the phosphatidylglycerol (PG) and cardiolipin (CL) of the bacterial membrane, thereby disrupting the cell membranes and allowing increased reactive oxygen species (ROS) as well as protein and DNA leakage. The results indicate that these neolignan-AMP mimic conjugates could be promising antimicrobial candidates for combating MRSA infections.
α-Santonin is a non-food naturally occurring sesquiterpene lactone, mainly derived from the Artemisia species. Biological activities of α-santonin and its derivatives have been extensively studied, ...including anticancer, anti-inflammatory, immunomodulation, antioxidant, antifungal, antipyretic and insecticidal activities. This review focused on plant resources and structural modifications of α-santonin, and chemical synthesis and bioactivities of α-santonin and its derivatives. Moreover, this review would provide important information for further research on α-santonin as a natural resource for applications in the agricultural and pharmaceutical industries.
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•α-Santonin, mainly isolated from Artemisia species, is a sesquiterpene lactone.•The method of total synthesis of α-santonin was comprehensively presented.•Structural modifications of α-santonin were summarized.•α-Santonin and its derivatives possessed various biological activities.
Infections caused by multidrug-resistant (MDR) bacteria are increasing worldwide, and with limited clinically available antibiotics, it is urgent to develop new antimicrobials to combat these MDR ...bacteria. Here, a class of novel amphiphilic xanthohumol derivatives were prepared using a building-block approach. Bioactivity assays showed that the molecule IV15 not only exhibited a remarkable antibacterial effect against clinical methicillin-resistant Staphylococcus aureus (MRSA) isolates (MICs: 1–2 μg/mL) but also had the advantages of rapid bactericidal properties, low toxicity, good plasma stability, and not readily inducing bacterial resistance. Mechanistic studies indicated that IV15 has good membrane-targeting ability and can bind to phosphatidylglycerol and cardiolipin in bacterial membranes, thus disrupting the bacterial cell membranes and causing increased intracellular reactive oxygen species and leakage of proteins and DNA, eventually resulting in bacterial death. Notably, IV15 exhibited remarkable in vivo anti-MRSA efficacy, superior to vancomycin, making it a potential candidate to combat MRSA infections.
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In continuation of our program aimed at the development of natural product-based pesticidal agents, a series of isoxazoline-containing ...podophyllotoxin/2′(2′,6′)-(di)halogenopodophyllotoxin derivatives were prepared, and their structures were well characterized by 1H NMR, IR, optical rotation, HRMS and mp. Especially the structure of compound Ia was further confirmed by 1H–1H COSY and NOESY spectrum. Among them, two compounds showed good insecticidal and acaricidal activities against Mythimna separata and Tetranychus cinnabarinus. Their structure–activity relationships were also observed.
Natural products are an abundant and environmentally friendly source for controlling plant pathogens and insect pests. Toward the development of new natural product-based pesticides, here, a series ...of osthole-based isoxazoline derivatives were prepared by 3 + 2 annulation and evaluated for their insecticidal activities and toxicities. The structures of all osthole-based isoxazoline derivatives were characterized by various spectral analyses, and derivative B13 was further confirmed by X-ray crystallography. Among all the osthole derivatives, B2 displayed the most promising growth inhibitory effect on Mythimna separata with a final corrected mortality rate of 96.4% ± 3.3, which was 1.80 times higher than those of both osthole and toosendanin. Derivative B13 displayed the most promising larvicidal activity against Plutella xylostella with an LC50 value of 0.220 mg/mL, which was superior to rotenone. Furthermore, both B13 and B21 also exhibited better control efficacy against P. xylostella than rotenone in the pot experiments. Additionally, the toxicity evaluation suggested that these osthole-based isoxazoline derivatives showed relatively low toxicity toward nontarget organisms. Given these results, osthole derivatives B2, B13, and B21 could be deeply developed as natural insecticidal agents in agriculture.
Toward the search of new antibacterial agents to control methicillin-resistant Staphylococcus aureus (MRSA), a class of new norfloxacin-1,3,4-oxadiazole hybrids were designed and synthesized. ...Antibacterial activities against drug-sensitive bacteria S. aureus and clinical drug resistant isolates of MRSA were evaluated. Compound 5k exhibited excellent antibacterial activities against S. aureus (MIC: 2 μg/mL) and MRSA1–3 (MIC: 0.25–1 μg/mL). The time-kill kinetics demonstrated that compound 5k had an advantage over commonly used antibiotics vancomycin in killing S. aureus and MRSA. Moreover, compound 5k could inhibit the bacteria and destroy their membranes in a short time, and showed very low cytotoxicity to NRK-52E cells. Some interesting structure-activity relationships (SARs) were also discussed. These results indicated that these norfloxacin-1,3,4-oxadiazole hybrids could be further developed into new antibacterial agents against MRSA.
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Due to their structural diversity and biological characteristics, natural products appear to be received much attention as lead compounds. Podophyllotoxin, a naturally sustainable aryltetralin ...lignan, is isolated from the roots and rhizomes of Podophyllum hexandrum. To discover new potentially natural product-based pesticidal agents, a series of isoxazole esters were regioselectively prepared by structural modification of podophyllotoxin. Compared with their precursor podophyllotoxin, compounds IId, IIIc and IIId exhibited the potent insecticidal activity, and compounds IIb, IIc, IIIc and IIId showed the pronounced acaricidal activity; especially compounds IIIc (X = Cl, R = 4-ClC6H4) and IIId (X = Cl, R = 4-FC6H4) exhibited the most promising pesticidal activities against Mythimna separata Walker and Tetranychus cinnabarinus Boisduval.
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•A series of isoxazole esters were regioselectively prepared by structural modification of podophyllotoxin.•Analogs IId, IIIc and IIId exhibited potent the insecticidal activity of their precursor podophyllotoxin.•Analogs IIb, IIc, IIIc and IIId showed the pronounced acaricidal activity of podophyllotoxin.•Analogs IIIc and IIId exhibited the most potent insecticidal and acaricidal activities against Mythimna separata and Tetranychus cinnabarinus.
To improve the insecticidal activity of (+)-nootkatone, a series of 42 (+)-nootkatone thioethers containing 1,3,4-oxadiazole/thiadiazole moieties were prepared to evaluate their insecticidal ...activities against Mythimna separata Walker, Myzus persicae Sulzer, and Plutella xylostella Linnaeus. Insecticidal evaluation revealed that most of the title derivatives exhibited more potent insecticidal activities than the precursor (+)-nootkatone after the introduction of 1,3,4-oxadiazole/thiadiazole on (+)-nootkatone. Among all of the (+)-nootkatone derivatives, compound 8c (1 mg/mL) exhibited the best growth inhibitory (GI) activity against M. separata with a final corrected mortality rate (CMR) of 71.4%, which was 1.54- and 1.43-fold that of (+)-nootkatone and toosendanin, respectively; 8c also displayed the most potent aphicidal activity against M. persicae with an LD50 value of 0.030 μg/larvae, which was closer to that of the commercial insecticidal etoxazole (0.026 μg/larvae); and 8s showed the best larvicidal activity against P. xylostella with an LC50 value of 0.27 mg/mL, which was 3.37-fold that of toosendanin and slightly higher than that of etoxazole (0.28 mg/mL). Furthermore, the control efficacy of 8s against P. xylostella in the pot experiments under greenhouse conditions was better than that of etoxazole. Structure–activity relationships (SARs) revealed that in most cases, the introduction of 1,3,4-oxadiazole/thiadiazole containing halophenyl groups at the C-13 position of (+)-nootkatone could obtain more active derivatives against M. separata, M. persicae, and P. xylostella than those containing other groups. In addition, toxicity assays indicated that these (+)-nootkatone derivatives had good selectivity to insects over nontarget organisms (normal mammalian NRK-52E cells and C. idella and N. denticulata fries) with relatively low toxicity. Therefore, the above results indicate that these (+)-nootkatone derivatives could be further explored as new lead compounds for the development of potential eco-friendly pesticides.
