Reactions of Heterocyclic beta-enaminoester, Synthesis and Antimicrobial Activity of Novel PyrimidinoPyrimidine Derivatives

In this work the corresponding 4-amino-6-pyridyl-2-phenyl-5-carbethoxypyrimidine (3) was synthesized through a one-pot, three-component reaction of pyridine-3-carbaldehyde, ethyl cyanoacetate and benzamidine hydrochloride in the presence of TEA in refluxing ethanol-DMF mixture. The synthesized pyrimidine (3) was directly transformed to medicinally important pyrimido[4,5-d]pyrimidine derivatives. All the synthesized products were tested and evaluated as antimicrobial agents. Keywords: Pyrimidine-5-ethyl carboxylate derivative, Pyrimido[4,5-d]pyrimidine, Chloroacetyl chlorid

Synthesis, characterization, biological activity, molecular docking and thermal analysis of binuclear complexes

ABSTRACT. Because of their potential medical applications as antimicrobial medicines, metal-ligand complexes have sparked a lot of attention. Synthesis and characterization of various metal-diamine complexes were the goals of the research detailed in this paper. As a result, synthesis of new binuclear ligand; N,N'-bis(3-carboxysalcylidene)-4-chloro-1,2-phenylenediamine (H4fsacph) which is derivative from the condensation of 3-formyl-2-hydroxybenzoic acid and 4-chlorobenzene-1,2-diamine has been performed. The new synthesized ligand has formed a mononuclear complex with Cu(II). The mononuclear Cu(II) complex was used to form binary nuclear complexes with some metal ions, like Cr(III), Mn(II), Fe(III), Ru(III), Pd(II) and La(III) ions. Elemental analysis, IR, UV-Visible, and thermal analyzes have been used to characterize the complexes. The interaction of a ligand with the receptors of Candida albicans and SARS-CoV-2 was predicted using molecular docking. Toward bacteria and fungi showing predominant activity against all fungi verified antibacterial activity of the synthesized complexes, while they have almost no activity against all bacteria. All compounds have shown antibacterial and antifungal activities, but the metal complexes showed better activities as compared to the original ligands, especially all zinc(II) complexes. The above results suggest that both ligands and their metal complexes have the potential to be explored as active pharmaceutical agents.   KEY WORDS: Molecular structure, Metal complexes, Molecular docking, Antimicrobial, SARS-CoV-2, Antifungal Bull. Chem. Soc. Ethiop. 2022, 36(4), 843-858.                                                             DOI: https://dx.doi.org/10.4314/bcse.v36i4.10                                                    &nbsp

EXISTENCE AND UNIQUENESS RESULTS FOR A COUPLED SYSTEM OF HADAMARD FRACTIONAL DIFFERENTIAL EQUATIONS WITH MULTI-POINT BOUNDARY CONDITIONS

In this paper, we have studied existence and uniqueness of solutions for a coupled system of multi-point boundary value problems for Hadamard fractional differential equations. By applying principle contraction and Shaefer's fixed point theorem new existence results have been obtained

Synthesis, mass spectroscopic studies, cytotoxicity evaluation and quantitative structure activity relationship of novel isoindolin-1,3-dione derivatives

3-Amino-4,6-diphenyl-2H-pyrazolo[3,4-b]pyridine (5) was synthesized as starting material and investigated as cytotoxic and antitumor agent. Compound 5 reacted with different acid anhydrides to afford the corresponding imides and bisimide derivatives 6-12. Imides 6-12 were tested for their in vitro cytotoxicity against four different cancer cell lines and structure activity relationship’s (SAR’s) was studied. Keywords: 2-Thiomethyl-4,6-diphenyl-3-carbonitrilpyridine, Acid Anhydrides, Cytotoxicity

Augmentation de l'effet de la psychothérapie par Amorçage Préconscient dans la phobie sociale et l’anxiété généralisée

Deux articles ont été publiés suite à ce mémoire de maîtrise. Un prix pour la meilleure affiche faite par un étudiant du département de psychiatrie de l'Universtité de Montréal a été obtenu suite à la présentation de résultats préliminaires à la Journée annuelle du Centre de recherche de l’Institut Universitaire en santé mentale de Montréal. Un support financier et des bourses ont été également accordés. Par exemple: Bourse d’excellence pour la recherche en psychiatrie, bourse du Cinquantenaire, Faculté de médecine, Département de psychiatrie, Université de Montréal; Bourse d’excellence du directeur de recherche, Centre d’études sur les troubles obsessionnels compulsifs et les tics- CETOCT; Centre recherche de l’Institut universitaire en santé mentale de Montréal; Bourse de Dépannage de la Faculté de médecine ainsi qu'une bourse de rédaction, Faculté de médecine de l’Université de Montréal, Montréal (QC).Les troubles anxieux représentent les problèmes de santé mentale les plus répandus. Ils affectent 12% de la population, causent un handicap léger à grave et peuvent représenter un lourd fardeau pour les patients et leurs proches. Ils entrainent un impact économique majeur pour la société en termes d’utilisation accrue des services de santé tant psychiatriques que non psychiatriques, de diminution de productivité au travail, d’absentéisme et du chômage. Cette étude de type série de cas, décrit une stratégie d’augmentation ou de facilitation du changement en psychothérapie basée sur l’amorçage (priming) préconscient et son utilisation dans le traitement de huit patients souffrant de troubles anxieux. Les patients avaient manifesté une réponse symptomatique partielle à la thérapie cognitive-comportementale (TCC) malgré une bonne adhésion au traitement. La démarche d’augmentation de la psychothérapie par amorçage préconscient (APAP) comporte six étapes permettant d’établir des formulations cognitives adaptées à la problématique résiduelle personnelle du patient. Ces formulations sont enregistrées et masquées par une musique relaxante. Les patients ont écouté cet enregistrement dans un état d’inattention pendant 20 minutes deux fois par jour durant huit semaines. L’effet de cette stratégie a été évalué par des mesures de type quantitatif et qualitatif, des mesures auto rapportées par les patients par rapport aux changements cognitifs idiosyncratiques ainsi que par un questionnaire sur la qualité de vie. Les résultats élaborés par une analyse descriptive incluant une exploration de la signification statistique et clinique des effets observés montrent, que la stratégie d’amorçage préconscient est associée à des changements cognitifs favorables, à une diminution du discours intérieur négatif et problématique chez sept patients sur huit. Ces bienfaits ont été également maintenus à la 24ème semaine. Une nette amélioration clinique des symptômes anxieux et du fonctionnement global a été observée chez deux patients qui souffraient uniquement d’un trouble anxieux versus les six autres qui présentent une comorbidité additionnelle à leur diagnostic primaire. Ces derniers ont quand même vu une amélioration de leur qualité de vie comparativement à leur état avant de recevoir la stratégie APAP. L’émergence de pensées et d’attitudes positives et la diminution des pensées dysfonctionnelles observées chez la majorité des patients à la suite du traitement par APAP, suggère un impact favorable de l’intervention. La démarche APAP qui est accessible par Internet pourrait constituer un ajout au traitement par TCC en facilitant ou en augmentant le changement cognitif et symptomatique.Anxiety disorders represent some of the most common mental health problems. These disorders affect up to 12% of the population causing mild to severe impairment and a potentially heavy burden for patients and their families. In addition, these disorders have a major economic impact on society in terms of increased use of health services both psychiatric and non- psychiatric, lower work productivity, absenteeism and unemployment. The current paper is a case series describing a new method for facilitating change based on Psychotherapy Augmentation through Preconscious Priming (APAP) and its use in the treatment of eight patients suffering from an anxiety disorder. Previously, the patients had shown only a partial response to CBT despite good adherence to treatment. Following this treatment, the patients completed the APAP process, which consisted of six steps during which alternative, more functional thoughts and beliefs were formulated, relevant to the idiosyncratic difficulties experienced by the patients. Subsequently, these formulations were recorded and mixed with masking relaxing music, following which the patient listened to the recordings in a passive state twice daily for 20 minutes for a period of 8 weeks. The effect of this strategy was evaluated by quantitative and qualitative measures administered before treatment with the APAP program, at 8 weeks, 16 weeks and 24 weeks. In addition, idiosyncratic ratings of dysfunctional thoughts, symptoms of anxiety, global functioning and quality of life were assessed at baseline and at 24 weeks. Results showed a significant reduction in dysfunctional thoughts reported by most patients treated with this method. There was substantial clinical improvement in anxiety symptoms both for patients who presented with and without co-morbid psychological disorders. Those with co-morbid psychological disorders who did not have a good quality of life at the start of treatment reported an increase in quality of life following treatment with APAP. In addition, a descriptive analysis of the results supported the notion that a preconscious priming strategy is associated with positive cognitive change with a reduction in negative thoughts in 7 out of 8 patients, which were maintained in the longer term. Further, this descriptive analysis suggested that patients who suffered from an anxiety disorder without co-morbidity showed more clinically significant improvement in anxiety symptoms and improved global functioning in comparison to those who presented with a co-morbid disorder. Overall, results suggested that the APAP intervention had a positive impact on the patients. Results showed that APAP led to positive cognitive changes in all patients and clinically significant improvement in anxiety symptoms and global functioning in patients without additional comorbidities. APAP could be a valuable addition to CBT by facilitating or enhancing cognitive and symptom change

Rôle des facteurs de virulence des Escherichia coli pathogènes aviaires dans la colibacillose

Thèse numérisée par la Direction des bibliothèques de l'Université de Montréal

Elitenformierung und Elitenwandel im Prozess der sudanesischen Nationenbildung

Diese Dissertationsarbeit untersucht Elitenformung und -wandel im Prozess der sudanesischen Nationenbildung. Angesichts des herrschenden Krieges im Land2, der seit der Unabhängigkeit des modernen Staates Sudan bis heute andauert, wird der Versuch unternommen, die Rolle der Elite bei den Kriegen und Unruhen im Land herauszufinden3. Dabei ist die Entwicklung von Eliten und deren Transformierung das Ziel der Untersuchung. Außerdem beschäftigt sich die Arbeit mit den Kommunikationsmitteln zwischen Eliten. Um diesen Entwicklungsprozess genauer nachvollziehen zu können, werden die historischen Entwicklungen, etwa wie die Kolonialära4 vorgestellt und deren Rolle bei der Entwicklung von sudanesischen Eliten bearbeitet. Dabei wird die Zeit von Muhammad Ali Pasha bis 2005 behandelt. Die vorliegende Untersuchung wird sich auf politische und wirtschaftliche Elite beschränken. Die Arbeit gliedert sich in neun Kapitel. Der erste Teil besteht aus einer Einführung in das Thema und den zu Grunde liegenden theoretischen Annahmen. Der Hauptteil beschäftigt sich mit dem Prozess der Nationenbildung im Sudan von den ersten Anfängen bis zur Gegenwart. Hierbei wird in größere Zeitabschnitte unterteilt. Die einzelnen Zeitabschnitte werden dann nach den folgenden Kriterien untersucht: erstens der gesellschaftlichen und politischen Lage (zu der Zeit), der politischen Führungselite und den jeweiligen Faktoren, die in dieser Etappe der Entwicklung Einfluss auf die Elitenformierung hatten, so etwa der Zugang zu Bildungsmöglichkeiten, der Einfluss der Religion und die Kriegs- oder Friedenssituation. Weiterhin werden einzelne Führungspersönlichkeiten als Vertreter der Elite herausgegriffen und biographisch kurz vorgestellt

Design and implementation of band rejected antennas using adaptive surface meshing and genetic algorithms methods. Simulation and measurement of microstrip antennas with the ability of harmonic rejection for wireless and mobile applications including the antenna design optimisation using genetic algorithms.

With the advances in wireless communication systems, antennas with different shapes and design have achieved great demand and are desirable for many uses such as personal communication systems, and other applications involving wireless communication. This has resulted in different shapes and types of antenna design in order to achieve different antenna characteristic. One attractive approach to the design of antennas is to suppress or attenuate harmonic contents due to the non-linear operation of the Radio Frequency (RF) front end. The objectives of this work were to investigate, design and implement antennas for harmonic suppression with the aid of a genetic algorithm (GA). Several microstrip patch antennas were designed to operate at frequencies 1.0, 1.8 and 2.4 GHz respectively. The microstrip patch antenna with stub tuned microstrip lines was also employed at 1.0 and 1.8 GHz to meet the design objectives. A new sensing patch technique is introduced and applied in order to find the accepted power at harmonic frequencies. The evaluation of the measured power accepted at the antenna feed port was done using an electromagnetic (EM) simulator, Ansoft Designer, in terms of current distribution. A two sensors method is presented on one antenna prototype to estimate the accepted power at three frequencies. The computational method is based on an integral equation solver using adaptive surface meshing driven by a genetic algorithm. Several examples are demonstrated, including design of coaxially-fed, air-dielectric patch antennas implanted with shorting and folded walls. The characteristics of the antennas in terms of the impedance responses and far field radiation patterns are discussed. The results in terms of the radiation performance are addressed, and compared to measurements. The presented results of these antennas show a good impedance matching at the fundamental frequency with good suppression achieved at the second and third harmonic frequencies.Home governmen

Segmented filamentous bacteria-based treatment to elicit protection against Enterobacteriaceae in Layer chickens

IntroductionGut microbes like segmented filamentous bacteria (SFB) play a key role in gut maturation during early life, as demonstrated in humans and mice. Our previous study demonstrated oral inoculation of ileum-spores containing SFB to chickens after hatch increases early SFB gut colonization, which increases immune maturation and resistance to bacteria, like Salmonella, as tested in vitro; however, more studies are needed for treatment optimization and in vivo testing. The objectives of this study were to (1) test a treatment that includes both spores and filamentous SFB, (2) validate antimicrobial ability of the treatment in layer hens in vivo, and (3) elucidate its molecular mechanism.MethodsOne-day-old specific pathogen-free layers (n = 12 per group) were orally treated with either PBS (CON) or SFB-based treatment (SFB). At 4 days post-inoculation (DPI), both CON and SFB groups were orally challenged with Salmonella Typhimurium. Total Enterobacteriaceae and Salmonella were examined by plating and enumeration in feces at 7,10 and 14 dpi; and in the ileum, cecum, and spleen at 16 dpi in euthanized birds. The presence and levels of SFB were determined from ilea scrapings via microscopy and qPCR, respectively. Relative gene expression of host-derived antimicrobial peptides and cytokines in the distal ileum was determined by RT-qPCR.ResultsAt 10 and 14 dpi, a significant decrease in total Enterobacteriaceae was observed in the feces of the SFB group. At necropsy, the level of SFB was significantly higher in the SFB group than in the CON group, while a significant decrease in total Enterobacteriaceae and Salmonella was observed in the ceca of the SFB group. RT-qPCR revealed increased expression of β-defensin 14, and cytokines IL-10 and IFNγ.DiscussionThe introduction of SFB at hatch as a prophylactic treatment may benefit commercial partners as well as consumers by reducing the incidence of Enterobacteriaceae in food animals. Reduction of these bacteria in animals would, in turn, increase animal health, productivity, and safety for consumers. Studies to optimize the treatment for poultry industry applications are ongoing in our lab

Harmonic-suppression Using Adaptive Surface Meshing and Genetic Algorithms

yesA novel design strategy for microstrip harmonic-suppression antennas is presented. The computational method is based on an integral equation solver using adaptive surface meshing driven by a genetic algorithm. Two examples are illustrated, all involving design of coaxially-fed air-dielectric patch antennas implanted with shorting and folded walls. The characteristics of the antennas in terms of the impedance responses and far ¯eld radiation patterns are discussed theoretically and experimentally. The performances of all of the GA-optimised antennas were shown to be excellent and the presented examples show the capability of the proposed method in antenna design using GA.MSCR