Novel,Dual Target-Directed Annelated Xanthine Derivatives Acting on Adenosine Receptors and Monoamine Oxidase B

Annelated purinedione derivatives have been shown to act as possible multiple-target ligands, addressing adenosine receptors and monoaminooxidases. In this study, based on our previous results, novel annelated pyrimido- and diazepino[2,1-f]purinedione derivatives were designed as dual-target-directed ligands combining A_2A adenosine receptor (AR) antagonistic activity with blocking monoamine oxidase B. A library of 19 novel compounds was synthesized and biologically evaluated in radioligand binding studies at AR subtypes and for their ability to inhibit MAO-B. This allowed 9-(2-chloro-6-fluorobenzyl)-3-ethyl-1-methyl-6,7,8,9-tetrahydropyrimido[2,1-f]purine-2,4(1H,3H)-dione ( 13 e ; K_i human A_2AAR: 264 nM and IC₅₀ human MAO-B: 243 nM) to be identified as the most potent dual-acting ligand from this series. ADMET parameters were estimated in vitro, and analysis of the structure-activity relationships was complemented by molecular-docking studies based on previously published X-ray structures of the protein targets. Such dual-acting ligands, by selectively blocking A_2A AR, accompanied by the inhibition of dopamine metabolizing enzyme MAO-B, might provide symptomatic and neuroprotective effects in, among others, the treatment of Parkinson disease     

梅塞斯米特Bf-109 G-6

<正>DiORAMA1/32介绍我的朋友邀请我制作一架豪普特曼·格尔哈德·巴克霍隆(Hauptmann Gerhard Barkhorn)驾驶的Bf-109 G-6。他希望把整架飞机安置在一个草坪地台之上,旁边站着它的机师。飞机涂装需要根据历史照片精确还原。我选用了长谷川出品的1/32 Bf-109,另外还添加了Master Details为本套材出品的树脂座舱、排气管、螺旋桨以及起落架组件,RB出品的蚀刻片,     

Learning semantically-annotated routes for context-aware recommendations on map navigation systems

Modern technology has brought many changes to our everyday lives. Our need to be in constant touch with others has been met with the cellphone, which has become our companion and the convergence point of many technological advances. The combination of capabilities such as browsing the Internet and GPS reception has multiplied the services and applications based on the current location of the user. However, providing the user with these services has certain drawbacks. Although map navigation systems are the most meaningful way of displaying this information, the user still has to manually set up the filter in order to obtain a non-bloated visualization of the map and the available services. To tackle this problem, we present here a semantic multicriteria ant colony algorithm capable of learning the user's routes, including associated context information, and then predicting the most likely route a user is following, given his current location and context data. This knowledge could then be used as the basis for offering services related to his current (or most likely future) context data close to the path he is following. Our experimental results show that our algorithm is capable of obtaining consistent solutions sets even when multiple objective ontological terms are included in the process.     

Rapid Models for Predicting the Low‐Temperature Behavior of Diesel

The cold filtration plugging point (CFPP) is the method most commonly applied to characterize the low‐temperature behavior of diesel and its components. However, this method is time‐consuming and does not have good repeatability, especially for samples with very low CFPP values like kerosene, light cycle oil, etc. Three new models for CFPP prediction were developed and compared: a combined density and distillation curve, differential scanning calorimetry, and near‐infrared. A set of 133 samples of diesel components were used to create the models, containing streams from different sources and levels of treatment. A further 28 diesel samples were used to validate and compare the models. All three models not only were faster than the standard method but also were found to be in good agreement with CFPP values. Each model has its own particular advantages suiting it to a particular type of diesel sample and stage of the diesel production process.     

Photocatalysis of xenobiotic organic compounds in greywater using zinc oxide nanoparticles: a critical review

The direct discharge of raw bathroom greywater has increased the concentrations of various pollutants in the water bodies. Typically, greywater contains large quantities of xenobiotic organic compounds (XOCs) owing to an increase in consumption of personal care and bath products. Therefore, it urges for a suitable technology to eliminate these compounds from contaminated waters. Photocatalytic degradation using Zinc Oxide nanoparticles (ZnO NPs) has the potentiality to eliminate various XOCs. However, ZnO NPs have high tendency to aggregate, which may lower the photocatalytic degradation rate. Therefore, there is an urgency to modify ZnO NPs to overcome the limitation. The present review was conducted to determine a suitable method for the modification ZnO NPs. Besides, the potential of the modified ZnO NPs in degrading XOCs in greywater as a photocatalyst was also discussed.     

Food security: perspectives from the Arab World

Editorial

Acknowledgement of reviewers     

Is unilateral breast enlargement always a sign of cancer?

Breast swelling is caused by many etiological factors, but should alert central vein occlusion in hemodialysis patients when the permanent vascular access is in the same arm. The swelling of the breast is caused by venous hypertension in the venous plexus draining the breast. Endovascular treatment relieves venous hypertension and related clinical signs. Additional diagnostic workup or invasive interventions such as a biopsy should be avoided in such patients, as diagnosis is straightforward with the presence of a functioning arteriovenous fistula in the same arm.     

Entropy-based feature selection for improved 3D facial expression recognition

Facial expressions contain most of the information on human face which is essential for human–computer interaction. Development of robust algorithms for automatic recognition of facial expressions with high recognition rates has been a challenge for the last 10 years. In this paper, we propose a novel feature selection procedure which recognizes basic facial expressions with high recognition rates by utilizing three-Dimensional (3D) geometrical facial feature positions. The paper presents a system of classifying expressions in one of the six basic emotional categories which are anger, disgust, fear, happiness, sadness, and surprise. The paper contributes on feature selections for each expression independently and achieves high recognition rates with the proposed geometric facial features selected for each expression. The novel feature selection procedure is entropy based, and it is employed independently for each of the six basic expressions. The system’s performance is evaluated using the 3D facial expression database, BU-3DFE. Experimental results show that the proposed method outperforms the latest methods reported in the literature.     

Generation of free radicals in partial oxidation of coal

Pyrolytic and oxidative treatments of two coals, Illinois No. 6 and Montour, have been performed between 140 and 400 °C. Free radical concentrations were followed by electron paramagnetic resonance as a function of time of treatment at a given temperature. Initial increases in the organic free radical concentrations were observed at all temperatures, but at the higher temperatures termination reactions caused the increase to be transient. Variations in the free radical concentrations of weathered and unweathered coal showed that the former produced a larger number of radicals. Possible effects due to native mineral matter are suggested.