New Fluorinated 1,2,4-Benzothiadiazine 1,1-Dioxides: Discovery of an Orally Active Cognitive Enhancer Acting through Potentiation of the 2-Amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic Acid Receptors

In the search of a potent cognitive enhancer, a series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as positive allosteric modulators of the AMPA receptors. In the present work, we focused our efforts on the insertion of mono- or polyfluoro- substituted alkyl chains at the 4-position of the thiadiazine ring in an attempt to enhance the pharmacokinetic behavior of previously described compounds. Among all the described compounds, 7-chloro-4-(2-fluoroethyl)-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide, 12b, was shown to exert a strong activity on AMPA receptors in vitro and a marked cognitive-enhancing effect in vivo after oral administration to Wistar rats. Considering its in vivo activity, the metabolic degradation of 12b was studied and compared to that of its nonfluorinated analogue 9b. Taken together, results of this study clearly validated the positive impact of the fluorine atom on the alkyl chain at the 4-position of benzothiadiazine dioxides on activity and metabolic stability

Autonomous space exploration using the Turtlebot mobile platform

Cilj diplomske naloge je implementacija avtonomnega raziskovanja prostora na mobilni platformi Turtlebot, ki uporablja razvojno okolje ROS. Implementirali smo raziskovalni algoritem, ki temelji na zaznavi obrobij in njihovi uporabi kot potencialnih raziskovalnih ciljev. Ker pa lahko algoritem pri izbiri raziskovalnih ciljev upošteva različne kombinacije ocen raziskovanja, smo nato preizkušali in primerjali, katera kombinacija ocen omogoča najbolj učinkovito raziskovanje prostora. Različne strategije izbire raziskovalnih ciljev smo ocenjevali in primerjali na podlagi štirih kriterijev ter referenčne strategije, ki naključno izbira raziskovalne cilje. Podatke za primerjavo smo dobili tako, da smo za vsako strategijo opravili deset uspešnih raziskovanj. Te smo nato kot skupine povprečnih vrednosti in odstopanj primerjali med seboj na podlagi referenčne strategije in kriterijev. Implementirali smo modul, ki poleg raziskanosti prostora in časa raziskovanja omogoča tudi beleženje zgodovine premikov in s tem pot raziskovanja, ki jo opravi Turtlebot.The purpose of this undergraduate thesis is to implement the autonomous exploration of space on the Turtlebot mobile platform that uses the ROS development environment. We implemented an exploration algorithm based on the detection and use of frontier regions as potential exploration goals. Since the algorithm is able to choose an exploration goal based on the combination of different assessments, we tested and compared which combination of goal assessments enables the most efficient exploration of a given space. We assessed and compared different strategies of goal setting on the basis of four criteria and a referential strategy which selects its exploration goals randomly. In order to get the data necessary for comparison, we conducted ten successful explorations per strategy and compared them on the basis of the referential strategy and criteria. We implemented our own module, which tracks the amount of space explored and the time spent for exploration, while also documenting the path traveled by the Turtlebot during exploration

Synthesis and Evaluation of New 6-formyl-oxazolo[3,2-a]pyrimidine derivatives as Potential Src Kinase Inhibitors

International audienc

Synthesis of 2-arylfuro[3,2-b]pyridines: Effect of the C2-aryl group on melatoninergic activity

International audienc

Preparation of cycloalkylated benzothiadiazine derivatives and their use as AMPA receptor modulators

publication date: 2009-07-07; filing date: 200