Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-Aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors

The synthesis and biological evaluation of novel 1-aryl-3-[2-, 3- or 4-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas 3, 4 and 5 as VEGFR-2 tyrosine kinase inhibitors, are reported. The 1-aryl-3-[3-(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas 4a-4h, with the arylurea in the meta position to the thioether, showed the lowest IC50 values in enzymatic assays (10-206 nM), the most potent compounds 4d-4h (IC50 10-28 nM) bearing hydrophobic groups (Me, F, CF3 and Cl) in the terminal phenyl ring. A convincing rationalization was achieved for the highest potent compounds 4 as type II VEGFR-2 inhibitors, based on the simultaneous presence of: (1) the thioether linker and (2) the arylurea moiety in the meta position. For compounds 4, significant inhibition of Human Umbilical Vein Endothelial Cells (HUVECs) proliferation (BrdU assay), migration (wound-healing assay) and tube formation were observed at low concentrations. These compounds have also shown to increase apoptosis using the TUNEL assay. Immunostaining for total and phosphorylated (active) VEGFR-2 was performed by Western blotting. The phosphorylation of the receptor was significantly inhibited at 1.0 and 2.5 microM for the most promising compounds. Altogether, these findings point to an antiangiogenic effect in HUVECs.

Myocardial perfusion by contrast echocardiography. Establishment of normal pattern of intracoronary injection and safety in humans

OBJECTIVE: To establish the normal pattern and safety of echocardiographic contrast in patients with no significant obstruction of epicardial coronary arteries. METHODS: 67 patients with normal coronary arteries or obstructions < 50% were selected from 277 patients who underwent coronary angiography (CA). Mean age was 56 ± 11years and 36 were males. At the end CA, echocardiographic contrast was selectively injected into each coronary artery. The parasternal short axis of the left ventricle (LV) was divided into six segments: anterior (A), antero-lateral (AL), postero-lateral (PL), posterior (P), infero-septal (IS) and antero-septal (AS). Anterolateral (ALPM) and posteromedial papillary muscles (PMPM) were also considered. The pattern and intensity of the appearance of the myocardial contrast was visually analyzed. RESULTS: The right coronary artery (RCA) was dominant in 60 patients. Contrast appearance was sudden and simultaneous in the 3 muscle layers. All segments could be contrasted after the injection in both coronary arteries. 100% of the AS, A and AL segments, 97% of the PL and 98% of the ALPM were perfused by the left coronary artery (LCA). P and IS segments were perfused by the RCA in 85% and 82%, respectively, and by a dominant LCA in 71% of the cases. The PMPM was perfused by a dominant RCA in 77% and by a dominant LCA in 86%. There were no symptoms. CONCLUSION: Intracoronary injection of the sonicated solution is a safe procedure that allows for an excellent opacification of the myocardium and can potentially be used during routine CA.

Anomalous origin of the left coronary artery from the right pulmonary artery with intramural aortic trajectory. Clinicosurgical diagnostic implications

OBJECTIVE: Anomalous origin of the left coronary artery from the right pulmonary artery (AOLCARPA), is a rare entity that is usually associated with other defects. Of the 20 cases of AOLCARPA reported in the literature, 14 (70%) had associations. We describe four patients with AOLCARPA without associated defects, but with a peculiar intramural aortic trajectory. METHODS: Fifty-five patients with anomalous origin of the left coronary artery were operated upon at INCOR-FMUSP. Four of the patients had the anomalous origin from the right pulmonary artery (RPA) without associated defects but with intramural aortic trajectory. Clinical and laboratory examinations were analyzed, as well as surgical findings. RESULTS: All patients had congestive heart failure (CHF) and 3 also had angina pectoris. Two patients had a murmur of mitral regurgitation, signs of myocardial infarction on the ECG and cardiomegaly. The shortening fraction varied from 9% to 23%. The hemodynamic study confirmed the diagnosis of anomalous origin of the coronary artery, but the intramural trajectory and the origin from the RPA were established only at surgery. In 3 patients, the technique of side-to-side anastomosis was performed with a good outcome. One patient, who underwent end-to-side anastomosis, died 6 months after the surgery. CONCLUSION: Association with other defects usually occurs in the AOLCARPA, and the intramural aortic trajectory is difficult to clinically diagnose but easy to surgically correct.

Hypertension in a female nursing staff-pattern of occurrence, diagnosis, and treatment

OBJECTIVE: To report the pattern of occurrence, diagnosis, and treatment of hypertension in a female nursing staff of an emergency hospital. METHODS: We carried out a cross-sectional study that included interviews and blood pressure measurements of 494 nursing professionals at an emergency hospital in the city of Salvador, in the state of Bahia, Brazil. We considered hypertensive all individual with blood pressure > or = 140/90 mmHg or normal pressure if on regular treatment. RESULTS: We found a prevalence of hypertension of 36.4%. Only 18.3% of the individuals ignored their hypertensive condition, and 64.2% admitted not being having regular treatment. Of those individuals who were having treatment, 69.4% had elevated blood pressure on examination. The major reasons for not being on treatment was the occasional elevation of blood pressure (22.2%) and medical counseling (20.0%). CONCLUSION: The results point to the need to introduce hypertension control measures in this occupational group, because of the magnitude of the disease and the potential impact on diffusion of knowledge and measures to control hypertension.

Development of a semi-automatic self learning pattern recognition system for the control of electronic boards

This project was funded under the Applied Research Grants Scheme administered by Enterprise Ireland. The project was a partnership between Galway - Mayo Institute of Technology and an industrial company, Tyco/Mallinckrodt Galway. The project aimed to develop a semi - automatic, self - learning pattern recognition system capable of detecting defects on the printed circuits boards such as component vacancy, component misalignment, component orientation, component error, and component weld. The research was conducted in three directions: image acquisition, image filtering/recognition and software development. Image acquisition studied the process of forming and digitizing images and some fundamental aspects regarding the human visual perception. The importance of choosing the right camera and illumination system for a certain type of problem has been highlighted. Probably the most important step towards image recognition is image filtering, The filters are used to correct and enhance images in order to prepare them for recognition. Convolution, histogram equalisation, filters based on Boolean mathematics, noise reduction, edge detection, geometrical filters, cross-correlation filters and image compression are some examples of the filters that have been studied and successfully implemented in the software application. The software application developed during the research is customized in order to meet the requirements of the industrial partner. The application is able to analyze pictures, perform the filtering, build libraries, process images and generate log files. It incorporates most of the filters studied and together with the illumination system and the camera it provides a fully integrated framework able to analyze defects on printed circuit boards.

SQL based frequent pattern mining

Data mining, frequent pattern mining, database mining, mining algorithms in SQL

Advancing the understanding of brain function with multivariate pattern analysis

Magdeburg, Univ., Fak. für Naturwiss., Diss., 2009

Optimization-based solutions to constrained trajectory-tracking and path-following problems

Magdeburg, Univ., Fak. für Elektrotechnik und Informationstechnik, Diss., 2012

Statistical pattern recognition for audio-forensics : empirical investigations on the application scenarios audio steganalysis and microphone forensics

Magdeburg, Univ., Fak. für Informatik, Diss., 2013

Citation-based Plagiarism Detection : applying citation pattern analysis to identify currently non-machine-detectible disguised plagiarism in scientific publications

Magdeburg, Univ., Fak. für Informatik, Diss., 2013

Robot trajectory optimization for relaxed effective tasks

Magdeburg, Univ., Fak. für Informatik, Diss., 2015

Spatio-temporal pattern formation in microemulsions under different physical and chemical conditions

Otto-von-Guericke-Universität Magdeburg, Fakultät für Naturwissenschaften, Dissertation, 2016

Ontogenetic variation of plastral spotting pattern in Phrynops hilarii (Testudines, Chelidae)

The plastral spotting variation in the chelid turtle Phrynops hilarii (Duméril & Bibron, 1835) in relation to sex, size, and geographic procedence of individuals was analyzed. States for qualitative characters were analyzed using non-parametric tests. Quantitative characters (shell and scute measurements) were standardized for body size by linear regression against carapace length, and were subjected to principal components analysis and canonical discriminant function analysis. Results suggest that increased plastral spotting is a polymorphic ontogenetic trait in P. hilarii. Neither hatchlings nor juveniles have plastral pattern moderately or heavily pigmented. The simplest pattern, however, may persist without changes in some adults. There are no differences between sexes. The spatial distribution of the plastral pattern is not ordered latitudinally or longitudinally, showing no relationship with gradients of elevation, temperature, or precipitation. This pattern trait lacks of taxonomic significance. The morphometric analysis failed to reveal any character of diagnostic utility in the plastron to support the possibility that these patterns correspond to different sympatric taxa.

The influence of shell species and size on the shell selection pattern of Paguristes tortugae (Decapoda, Diogenidae) from Anchieta Island (Ubatuba, Brazil)

Shell selection by the hermit crab Paguristes tortugae Schmitt, 1933 from Anchieta Island (Brazil) was analyzed using the six most frequently occupied shell species in the field and taking into account the sexual condition of the individuals, the shell size and the shell species. The experiments were conducted under laboratory conditions and the shell species preference was estimated on the basis of the frequency that each species was chosen by the individuals. The preferred shell species and size were determined by regression analysis. The highest correlation coefficients were obtained for the relations between the hermit dimensions and shell dry weight. The ovigerous females preferred shells with larger internal volume: Leucozonia nassa (Gmelin, 1791) and Cerithium atratum (Born, 1778). In the experiment of shell size, males preferred heavier shells whereas females selected the shape characteristics of the shell, such as the aperture and the internal volume, which are probably related to the growth and offspring guarantee, respectively. In general, and independent of sex condition, P. tortugae showed significant selection among all shells utilized. The results suggest that shell selection by P. tortugae involves sexual and reproductive condition preferences.

Shell utilization pattern of the hermit crab Clibanarius vittatus (Crustacea, Anomura) in an estuary at São Vicente, State of São Paulo, Brazil

We evaluated the gastropod shell utilization pattern of the hermit crab Clibanarius vittatus (Bosc, 1802) at Pescadores Beach in São Vicente, State of São Paulo, Brazil. Specimens were collected monthly from May 2001 through April 2003, in the intertidal zone at low tide. The crabs were weighed and their carapace shield length measured. All gastropod shells were identified and had their shell biometric parameters (total length and aperture length) measured (mm) and weighed (g). A total of 2,344 hermit crabs (644 males, 1,594 females, 45 ovigerous females and 61 individuals in intersex), using 13 species of gastropod shells, were collected. Stramonita haemastoma (Linnaeus, 1767), Cymatium parthenopeum (Von Salis, 1793) and Achatina fulica (Bowdich, 1822) comprised over 98% of all the shells. Male and intersex crabs were significantly larger than the females. This size difference strongly influenced the shell utilization pattern, principally in A. fulica, which has the largest shell size, that was only used by males and intersexual individuals of C. vittatus. Cymatium parthenopeum was the only shell species that showed a high determinant coefficient in all the biometric correlations evaluated. The high abundance of S. haemastoma shells and a strong correlation between crab size and shell aperture length established by a significant determination coefficient, indicated that C. vittatus uses this species as the principal resource for shell occupation at Pescadores Beach.