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How and to which extent terrain factors affecting the drainage area threshold (DAT) are disputable. This paper uses principal component analysis (PCA) and correlation analysis to study the influence degree of terrain factors on DAT. Firstly, 22 watersheds, locating in the severe soil erosion region (SSER) of Loess Plateau of China, are picked out as the example areas. The purpose of the mean change point method (MCP) to detect the relationship between DAT and gully density (GD) is to get a reasonable DAT. Secondly, nine terrain factors are calculated, and their statistical values are compared and put in the matrix to clear the different effects on DAT. Finally, the effects of statistical eigenvalues of terrain factors on DAT are compared with PCA and the correlation analysis. According to the PCA, the nine terrain factors are summarized into three principal components, which are slope, height variation, and relief factor. By calculating the score weighted by each factor coefficient matrix and eigenvalue, the result states that slope (S), terrain curvatures (K), and surface roughness (SR) are the factors that have great influence on DAT. Meanwhile, the results of correlation analysis indicate that S, SR, and K have exerted a great influence on the DAT, and the significance level was above 0.05. Both the results of PCA and correlation analysis make clear that the slope is the most direct and influential factor affecting DAT, while other factors are more or less related to slope directly and indirectly. The result implies that the vertical variation of terrain has a strong correlation with the slope, and also has a great influence on DAT. This research not only would be of great significance to recognize the mechanism of gully development, but also able to provide a scientific reference for soil and water conservation in the Loess Plateau.
Assuntos
Monitoramento Ambiental , Solo , China , Análise de Componente PrincipalRESUMO
Indoor robotic localization is one of the most active areas in robotics research nowadays. Visible light positioning (VLP) is a promising indoor localization method, as it provides high positioning accuracy and allows for leveraging the existing lighting infrastructure. Apparently, accurate positioning performance is mostly shown by the VLP system with multiple LEDs, while such strict requirement of LED numbers is more likely to lead to VLP system failure in actual environments. In this paper, we propose a single-LED VLP system based on image sensor with the help of angle sensor estimation, which efficiently relaxes the assumption on the minimum number of simultaneously captured LEDs from several to one. Aiming at improving the robustness and accuracy of positioning in the process of continuous change of robot pose, two methods of visual-inertial message synchronization are proposed and used to obtain the well-matched positioning data packets. Various schemes of single-LED VLP system based on different sensor selections and message synchronization methods have been listed and compared in an actual environment. The effectiveness of the proposed single-LED VLP system based on odometer and image sensor as well as the robustness under LED shortage, handover situation and background non-signal light interference, are verified by real-world experiments. The experimental results show that our proposed system can provide an average accuracy of 2.47 cm and the average computational time in low-cost embedded platforms is around 0.184 s.
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A series of new diarylpyrimidines (DAPYs) characterized by a halogen atom on the methylene linker between wing I and the central pyrimidine ring was synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures. The two most promising compounds 7f and 7g showed excellent activity against wild-type HIV-1 with low nanomolar EC50 values of 0.005 and 0.009 µM, respectively, which were comparable to or more potent than all the reference drugs zidovudine (AZT), lamivudine (3TC), nevirapine (NEV), efavirenz (EFV), delaviridine (DLV) and etravirine (ETV). In particular, 7g also displayed strong activity against the double mutant strain 103N + 181C with an EC50 value of 8.2 µM. The preliminary structure-activity relationship (SAR) and molecular docking analysis of this new series of CHX-DAPYs were also investigated.
Assuntos
Fármacos Anti-HIV/síntese química , Fármacos Anti-HIV/farmacologia , Benzamidas/síntese química , Benzamidas/farmacologia , Desenho de Fármacos , Transcriptase Reversa do HIV/antagonistas & inibidores , Pirimidinas/farmacologia , Inibidores da Transcriptase Reversa/síntese química , Inibidores da Transcriptase Reversa/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , HIV-1/efeitos dos fármacos , Humanos , Modelos Moleculares , Simulação de Acoplamento Molecular , Estrutura Molecular , Nitrilas , Leucemia-Linfoma Linfoblástico de Células Precursoras/tratamento farmacológico , Leucemia-Linfoma Linfoblástico de Células Precursoras/patologia , Leucemia-Linfoma Linfoblástico de Células Precursoras/virologia , Pirimidinas/síntese química , Pirimidinas/química , Relação Estrutura-Atividade , Células Tumorais Cultivadas , Replicação Viral/efeitos dos fármacosRESUMO
A series of CR2(OH)-diarylpyrimidine derivatives (CR2(OH)-DAPYs) featuring a hydrophobic group at CH(OH) linker between wing I and the central pyrimidine were synthesized and evaluated for their anti-HIV activity in MT-4 cell cultures. All the target compounds except for compound 3k displayed inhibitory activity against HIV-1 wild-type with EC50 values ranging from 7.21±1.99 to 0.067±0.006 µM. Among them, compound 3d showed the most potent anti-HIV-1 activity (EC50=0.067±0.006 µM, SI>592), which was approximately 2-fold more potent than the reference drugs nevirapine (NVP) and delaviridine (DLV) in the same assay. In addition, the binding modes with HIV-1 RT and the preliminary SAR studies of these new derivatives were also investigated.
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Transcriptase Reversa do HIV/antagonistas & inibidores , HIV-1/enzimologia , Inibidores da Transcriptase Reversa/química , Sítios de Ligação , Linhagem Celular , Transcriptase Reversa do HIV/metabolismo , Humanos , Simulação de Acoplamento Molecular , Estrutura Terciária de Proteína , Pirimidinas/química , Pirimidinas/metabolismo , Inibidores da Transcriptase Reversa/metabolismo , Relação Estrutura-AtividadeRESUMO
A series of C6-rigid S-DABO analogs characterized by a substituted benzoyl group at C6 position of the pyrimidine ring has been synthesized and biological evaluation as NNRTIs against wild-type HIV-1 strain IIIB, double RT mutant (K103N+Y181C) strain RES056 as well as HIV-2 strain ROD in MT-4 cell cultures. Most of the compounds exhibited moderate antiviral activities. Among them, compound 7q displayed the highest anti-HIV-1 activity with an EC50 value of 0.26µM and a selectivity index (SI) of 541. The preliminary structure-activity relationship (SAR) of these new S-DABOs was investigated, the target RT was confirmed and docking study was performed.
Assuntos
Transcriptase Reversa do HIV/antagonistas & inibidores , HIV-1/enzimologia , Pirimidinas/química , Pirimidinonas/síntese química , Inibidores da Transcriptase Reversa/síntese química , Sítios de Ligação , Transcriptase Reversa do HIV/metabolismo , Humanos , Simulação de Acoplamento Molecular , Ligação Proteica , Estrutura Terciária de Proteína , Pirimidinas/síntese química , Pirimidinas/metabolismo , Pirimidinonas/química , Pirimidinonas/metabolismo , Inibidores da Transcriptase Reversa/química , Inibidores da Transcriptase Reversa/metabolismo , Relação Estrutura-AtividadeRESUMO
A new efficient synthesis of pyrano[2,3-b]quinoline derivatives is developed via the H2SO4-mediated tandem cyclization/ring-opening/recyclization reaction of readily available 1-acetyl N-aryl cyclopentanecarboxamides, during which a novel ring-cleavage fashion of the cyclopentane unit is involved and possible mechanisms are discussed.
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Ciclopentanos/síntese química , Piranos/síntese química , Quinolinas/síntese química , Ciclização , Ciclopentanos/química , Estrutura Molecular , Piranos/química , Quinolinas/químicaRESUMO
This review discusses chiral-at-metal complexes and introduces enantiomorphs from assembly structure. Owing to the diverse coordination number and activity of metal ions as chiral centers, abundant structures for chiral selectivity, catalysis, and polarized light-response are the notable advantages of the chiral-at-metal complexes. The rational design and preparation of linear multi-dentate ligands is a good choice to improve the stability of chiral complexes, such as multi-bonding structure for high stability as a self-limiting system. The bio-significance and potential application of chiral-at-metal complexes are discussed, such as the synergistic effect of catalysis and chiral selectivity of the metal center in enzymes. Enzyme could be remolded to replace the original central metal ions with highly active rare earth or precious metal ions to form artificial metalloenzyme or to remove the "redundant" part around the metal center to improve the accessibility of substrate. The polarized light-response mechanism of chiral opsin is introduced in relation to its role in animal migration. Metal-organic frameworks (MOFs) are crystalline and porous materials built from metal nodes or clusters and organic linkers and provide the possibility to prepare artificial enantiomorphs. The preparations, applications, and characterization methods of MOF enatiomorphs are therefore introduced. We hope this review inspires researchers at all levels of their career to consider the title topic in their own research in terms of its application and potential value.
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A SnCl4.5H2O-mediated facile and efficient one-step synthesis of the tricyclic core of martinellic acid from readily available 2-(cyanomethyl)-3-oxo-N-arylbutanamides was developed and a mechanism involving consecutive hydrolysis of a cyano group and a double annulation process is proposed.