Behaviour of 4-(4-acetoaminophenyl)-4-oxobut-2-enoic acid towards carbon and nitrogen nucleophiles and use of these products in the synthesis of some interesting heterocycles

The present work is devoted to study the interaction of-aroylacrylic acid derivative (1) with some containing active methylene compounds under Michael reaction conditions and afforded the Michael adducts (2a-e). When compound 1 was allowed to react with cyclohexanone in the presence of ammonium acetate as catalyst, it afforded hydroquinoline derivative (3). Interaction of the acid 1 with highly and moderately reactive hydrocarbons e.g. p-xylene and acetanilide in the presence of anhydrous aluminumchloride under Friedel-Crafts reaction conditions afforded (4a-b). On the other hand, when the acid 1 was allowed to react with benzyl amine in dry benzene yielded 2-benzylamino-4-(4-acetaminophenyl)-4-oxobutanoic acid (5). This later compound was used to synthesize some heterocyclic compounds (7-11). Also, aza Michael adduct (6) used asthe key starting material for the synthesis of some interesting heterocyclic compounds e.g. pyridazinone, oxazinoneand furanone derivatives (13-16)

Utility of 4-(4-acetoaminophenyl)-4-oxo-but-2-enoic acid to prepare Pyranand Pyridine derivatives as building blocks in Heterocyclic Synthesis

The present work is devoted to study the interaction of β -aroylacrylic acid derivative (1) with malononitrile in the presence of piperidine and/or ammonium acetate, then using the formed compounds as a starting material for synthesizing fused and isolated heterocyclic system. Ithas been established that the β-aroylacrylic acid (1) reactwith malononitrile in (DMF) in the presence of piperidineas catalyst with formation of 4H-pyran derivative (2). Bychanging the catalyst into ammonium acetate, pyridine derivative (3) has been obtained. When compound (2) wasallowed to react with triethylorthoformate afforded ethoxymethyleneamino-4H-pyran (4). Compound (4) was used askey starting material for synthesizing some interesting annulated and heterocyclic systems (5-8). Also, the maleamic acid derivatives (9) and (15) have been synthesized via the interaction of (2) and (3) with maleic anhydride to study the behavior of the formed maleamic acid derivatives asanalogies of β-aroylacrylic towards different active methylene compounds under Michael addition reaction (10-14); (16-18)

North Atlantic right whale localization and recognition using very deep and leaky Neural Network

We describe a deep learning model that can be used to recognize individual right whales in aerial images. We developed our model using a data set provided by the National Oceanic and Atmospheric Administration. The main challenge we faced when working on this data set is that the size of the training set is very small (4,544 images) with some classes having only 1 image. While this data set is by far the largest of its kind, it is very di cult to train a deep neural network with such a small data set. However, we were able to overcome this challenge by dividing this problem into smaller tasks and by reducing the viewpoint variance in the data set. First, we localize the body and the head of the whale using deep learning. Then, we align the whale and normalize it with respect to rotation. Finally, a network is used to recognize the whale by analyzing its callosities. The top-1 accuracy of the model is 69.7% and the top-5 accuracy is 85%. The solution we describe in this paper was ranked 5th (out of 364 teams) in a challenge to solve this problem

A modified Block Matching 3D algorithm for additive noise reduction

This paper presents a patch-based image ltering algorithm for addi- tive noise reduction. Our algorithm is a modi cation to the block matching 3D algorithm, where an adaptive thresholding was used for the collaborative hard- thresholding step. The collaborative Wiener ltering step was also modi ed by assigning more weights for similar patches. Experimental results show that our algorithm outperforms the original block matching 3D algorithm at various noise levels

Lack of awareness of erectile dysfunction in many men with risk factors for erectile dysfunction

<p>Abstract</p> <p>Background</p> <p>Men with erectile dysfunction often have concurrent medical conditions. Conversely, men with these conditions may also have underlying erectile dysfunction. The prevalence of unrecognized erectile dysfunction in men with comorbidities commonly associated with erectile dysfunction was determined in men invited to participate in a double-blind, randomized, placebo-controlled trial of sildenafil citrate.</p> <p>Methods</p> <p>Men ≥30 years old presenting with ≥1 erectile dysfunction risk factor (controlled hypertension, hypercholesterolemia, smoking, metabolic syndrome, stable coronary artery disease, diabetes, depression, lower urinary tract symptoms, obesity [body mass index ≥30 kg/m²] or waist circumference ≥40 inches), and not previously diagnosed with erectile dysfunction were evaluated. The screening question, "Do you have erectile dysfunction?," with responses of "no," "yes," and "unsure," and the Erectile Function domain of the International Index of Erectile Function (IIEF-EF) were administered.</p> <p>Results</p> <p>Of 1084 men screened, 1053 answered the screening question and also had IIEF-EF scores. IIEF-EF scores indicating erectile dysfunction occurred in 71% (744/1053), of whom 54% (399/744) had moderate or severe erectile dysfunction. Of 139 answering "yes," 526 answering "unsure," and 388 answering "no," 96%, 90%, and 36%, respectively, had some degree of erectile dysfunction. The mean±SD (range) number of risk factors was 2.9 ± 1.7 (3-8) in the "yes" group, 3.2 ± 1.7 (3-9) in the "unsure" group, and 2.6 ± 1.5 (2-8) in the "no" group.</p> <p>Conclusion</p> <p>Although awareness of having erectile dysfunction was low, most men with risk factors had IIEF-EF scores indicating erectile dysfunction. Erectile dysfunction should be suspected and assessed in men with risk factors, regardless of their apparent level of awareness of erectile dysfunction.</p> <p>Trial registration</p> <p>ClinicalTrials.gov Identifier NCT00343200.</p

Determinants of male reproductive health disorders: the Men in Australia Telephone Survey (MATeS)

Background: The relationship between reproductive health disorders and lifestyle factors in middle-aged and older men is not clear. The aim of this study is to describe lifestyle and biomedical associations as possible causes of erectile dysfunction (ED), prostate disease (PD), lower urinary tract symptoms (LUTS) and perceived symptoms of androgen deficiency (pAD) in a representative population of middle-aged and older men, using the Men in Australia Telephone Survey (MATeS). Methods: A representative sample (n = 5990) of men aged 40+ years, stratified by age and State, was contacted by random selection of households, with an individual response rate of 78%. All men participated in a 20-minute computer-assisted telephone interview exploring general and reproductive health. Associations between male reproductive health disorders and lifestyle and biomedical factors were analysed using multivariate logistic regression (odds ratio [95% confidence interval]). Variables studied included age, body mass index, waist circumference, smoking, alcohol consumption, physical activity, co-morbid disease and medication use for hypertension, high cholesterol and symptoms of depression. Results: Controlling for age and a range of lifestyle and co-morbid exposures, sedentary lifestyle and being underweight was associated with an increased likelihood of ED (1.4 [1.1-1.8]; 2.9 [1.5-5.8], respectively) and pAD (1.3 [1.1-1.7]; 2.7 [1.4-5.0], respectively. Diabetes and cardiovascular disease were both associated with ED, with hypertension strongly associated with LUTS and pAD. Current smoking (inverse association) and depressive symptomatology were the only variables independently associated with PD. All reproductive disorders showed consistent associations with depression (measured either by depressive symptomatology or medication use) in both age-adjusted and multivariate analyses. Conclusion: A range of lifestyle factors, more often associated with chronic disease, were significantly associated with male reproductive health disorders. Education strategies directed to improving general health may also confer benefits to male reproductive health.Carol A. Holden, Robert I. McLachlan, Marian Pitts, Robert Cumming, Gary Wittert, Johnathon P. Ehsani, David M. de Kretser, David J. Handelsma

Effects of antiplatelet therapy on stroke risk by brain imaging features of intracerebral haemorrhage and cerebral small vessel diseases: subgroup analyses of the RESTART randomised, open-label trial

Background Findings from the RESTART trial suggest that starting antiplatelet therapy might reduce the risk of recurrent symptomatic intracerebral haemorrhage compared with avoiding antiplatelet therapy. Brain imaging features of intracerebral haemorrhage and cerebral small vessel diseases (such as cerebral microbleeds) are associated with greater risks of recurrent intracerebral haemorrhage. We did subgroup analyses of the RESTART trial to explore whether these brain imaging features modify the effects of antiplatelet therapy