Traditional DeepLabV3+ image semantic segmentation methods face challenges in pitaya orchard environments characterized by multiple interference factors, complex image backgrounds, high computational ...complexity, and extensive memory consumption. This paper introduces an improved visual navigation path recognition method for pitaya orchards. Initially, DeepLabV3+ utilizes a lightweight MobileNetV2 as its primary feature extraction backbone, which is augmented with a Pyramid Split Attention (PSA) module placed after the Atrous Spatial Pyramid Pooling (ASPP) module. This improvement enhances the spatial feature representation of feature maps, thereby sharpening the segmentation boundaries. Additionally, an Efficient Channel Attention Network (ECANet) mechanism is integrated with the lower-level features of MobileNetV2 to reduce computational complexity and refine the clarity of target boundaries. The paper also designs a navigation path extraction algorithm, which fits the road mask regions segmented by the model to achieve precise navigation path recognition. Experimental findings show that the enhanced DeepLabV3+ model achieved a Mean Intersection over Union (MIoU) and average pixel accuracy of 95.79% and 97.81%, respectively. These figures represent increases of 0.59 and 0.41 percentage points when contrasted with the original model. Furthermore, the model’s memory consumption is reduced by 85.64%, 84.70%, and 85.06% when contrasted with the Pyramid Scene Parsing Network (PSPNet), U-Net, and Fully Convolutional Network (FCN) models, respectively. This reduction makes the proposed model more efficient while maintaining high segmentation accuracy, thus supporting enhanced operational efficiency in practical applications. The test results for navigation path recognition accuracy reveal that the angle error between the navigation centerline extracted using the least squares method and the manually fitted centerline is less than 5°. Additionally, the average deviation between the road centerlines extracted under three different lighting conditions and the actual road centerline is only 2.66 pixels, with an average image recognition time of 0.10 s. This performance suggests that the study can provide an effective reference for visual navigation in smart agriculture.
TYK2 is a JAK family protein tyrosine kinase activated in response to multiple cytokines, including type I IFNs, IL-6, IL-10, IL-12, and IL-23. Extensive studies of mice that lack TYK2 expression ...indicate that the IFN-α, IL-12, and IL-23 pathways, but not the IL-6 or IL-10 pathways, are compromised. In contrast, there have been few studies of the role of TYK2 in primary human cells. A genetic mutation at the tyk2 locus that results in a lack of TYK2 protein in a single human patient has been linked to defects in the IFN-α, IL-6, IL-10, IL-12, and IL-23 pathways, suggesting a broad role for TYK2 protein in human cytokine responses. In this article, we have used a panel of novel potent TYK2 small-molecule inhibitors with varying degrees of selectivity against other JAK kinases to address the requirement for TYK2 catalytic activity in cytokine pathways in primary human cells. Our results indicate that the biological processes that require TYK2 catalytic function in humans are restricted to the IL-12 and IL-23 pathways, and suggest that inhibition of TYK2 catalytic activity may be an efficacious approach for the treatment of select autoimmune diseases without broad immunosuppression.
A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as psoriasis and inflammatory bowel diseases (IBD), by selective targeting of TYK2. Hit triage, following a ...high-throughput screen for TYK2 inhibitors, revealed pyridine 1 as a promising starting point for lead identification. Initial expansion of 3 separate regions of the molecule led to eventual identification of cyclopropyl amide 46, a potent lead analog with good kinase selectivity, physicochemical properties, and pharmacokinetic profile. Analysis of the binding modes of the series in TYK2 and JAK2 crystal structures revealed key interactions leading to good TYK2 potency and design options for future optimization of selectivity.
Display omitted
•Biological rationale for targeting selective TYK2 inhibition is given.•We report lead identification of potent and efficient TYK2 inhibitors.•Analogs afford modest selectivity against other Janus Family kinases.•We obtained crystal structures of key compounds bound to both TYK2 and JAK2.•ADME properties of the lead compound are favorable.
Herein we report our lead optimization effort to identify potent, selective, and orally bioavailable TYK2 inhibitors, starting with lead molecule 3. We used structure-based design to discover ...2,6-dichloro-4-cyanophenyl and (1R,2R)-2-fluorocyclopropylamide modifications, each of which exhibited improved TYK2 potency and JAK1 and JAK2 selectivity relative to 3. Further optimization eventually led to compound 37 that showed good TYK2 enzyme and interleukin-12 (IL-12) cell potency, as well as acceptable cellular JAK1 and JAK2 selectivity and excellent oral exposure in mice. When tested in a mouse IL-12 PK/PD model, compound 37 showed statistically significant knockdown of cytokine interferon-γ (IFNγ), suggesting that selective inhibition of TYK2 kinase activity might be sufficient to block the IL-12 pathway in vivo.
It is believed that β-amyloid aggregation is an important event in the development of Alzheimer’s disease. In the course of our studies to identify β-amyloid aggregation inhibitors, a series of
...N-phenyl anthranilic acid analogs were synthesized and studied for β-amyloid inhibition activity. The synthesis, structure–activity relationship, and in vivo activity of these analogs are discussed.
It is believed that β-amyloid aggregation is an important event in the development of Alzheimer’s disease. In the course of our studies to identify β-amyloid aggregation inhibitors, a series of
N-phenyl anthranilic acid analogs were synthesized and studied for β-amyloid inhibition activity. The synthesis, structure–activity relationship, and in vivo activity of these analogs are discussed.
Cu–ZrOx/SBA-15 catalyzes the aniline N-monomethylation using CO2 and H2 to produce methylaniline with 97.6% conversion and 96.5% selectivity.
Display omitted
•Cu–ZrOx composite is highly dispersed on ...SBA-15 for N-monomethylation reactions using CO2 and H2.•The optimal Cu–ZrOx/SBA-15 affords 97.6% aniline conversion and 96.5% N-methylaniline selectivity.•The catalytic performance of Cu–ZrOx/SBA-15 remains stable during cycles.•CO2 preferentially reacts with adsorbed aniline rather than direct hydrogenation.
N-methylation of amines using CO2 and H2 addresses the problems of expensive raw materials and harsh reaction conditions. However, designing a high-active and stable interface for the efficient preparation of monomethyl amine compounds in this tandem reaction remains a challenge to be overcome. Here, Cu–ZrOx composites are dispersed on SBA-15, silicalite-1, and ZSM-5 through the oxalic acid precipitation method for the N-methylation of amines using CO2 and H2. Results show that the dispersion of Cu–ZrOx on the surface of SBA-15 is superior to the other two molecular sieves and effectively prevents the sintering of active metals. A 20 wt% Cu–ZrOx/SBA-15 catalyst proves to be optimal for the N-methylation of aniline (AN) using CO2 and H2 to methylaniline (MA) and the catalyst performance remains stable after 5 cycle runs. The optimal catalyst exhibits an AN conversion of 97.6% and a selectivity of 96.5% for MA under the conditions of 180 °C, 4.0 MPa (H2/CO2/N2 = 72/24/4, molar ratio), and 8 h. Spectroscopic investigation and controlled experiments indicated that the preferential adsorbed AN on the catalyst surface reacts with CO2 to generate C–N bond, thereby avoiding the self-coupling side reaction of AN and achieving a high yield of 94.2% for MA.
We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses exceptional potency at MC4R and potent ...anti-obesity efficacy in a mouse model. However, the efficacy is not completely mediated through MC4R. Additional SAR studies led to the discovery of compound 32, which is more potent at MC4R. Compound 32 demonstrates MC4R mediated anti-obesity efficacy in rodent models.
We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses exceptional potency at MC4R and potent anti-obesity efficacy in a mouse model. However, the efficacy is not completely mediated through MC4R. Additional SAR studies led to the discovery of compound 32, which is more potent at MC4R. Compound 32 demonstrates MC4R mediated anti-obesity efficacy in rodent models.
One of the key issues in sustainable tourism research is the gap between tourists’ expressed friendly attitudes towards sustainable behaviors and their actual behaviors. Although many “low-carbon” ...themed restaurants have emerged during the low-carbon transformation of the Chinese tourism industry, low-carbon food services have not been significantly improved. This study takes food as the entry point to explore tourists’ behavior and attitudes towards low-carbon tourism in relation to food. We conducted two interviews. The first interview was a semi-structured contextual interview with 120 tourists who had experiences in food streets, aiming to identify the core user group: low-carbon attitude-friendly tourists with high-carbon food behaviors. The second interviews was an in-depth interview based on grounded theory with 29 core users, analyzing the four main reasons for their high-carbon food behaviors and their requirements for low-carbon food services in tourism. Based on this, we extracted four design elements for low-carbon tourism food services: low-carbon information show service, low-carbon service product attractiveness improvement, low-carbon food environment atmosphere creation, and service providers’ low-carbon behaviors. Through these four service elements, we constructed a low-carbon tourism food service design framework based on the core users’ needs, discussed the mechanism of service elements, and provided service design suggestions accordingly. The research results can be helpful for tourism providers, low-carbon tourism researchers, and designers.
With the introduction of “carbon neutrality”, promoting carbon peaking and carbon neutrality has become contingent upon the vigorous development of pure electric vehicles. The development of electric ...minivans is receiving substantial backing from the government as China’s logistics vehicle market undergoes a transformation. The drivers of electric minivans in China’s Shanxi Province are the objects of this research, whose purpose was to establish a service model based on the four elements of service design and grounded theory to clarify the key factors of user guarantee for electric minivans. We conducted a pilot study using questionnaires, user patterns, user interviews, and a user journey map to determine the user needs for electric minivan user service guarantees. NVivo was used to analyze and code the user interview data qualitatively. The research findings can serve as a resource for entrepreneurs, service providers, managers, and designers of electric minivans.
PDF
