Synthesis of substituted 3-anilino-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepine-2-ones and their evaluation as cholecystokinin-ligands

3-Amino-1,4-benzodiazepines as well as chemically related diverse amines were prepared from oxazepam and subsequently screened on the cholecystokinin receptor in a radiolabel binding assay. Oxazepam 2 was activated via its 3-chloro-1,4-benzodiazepine intermediate 3 and was reacted with a large series of aliphatic and aromatic amines. The substituted 3-anilino-1,4-benzodiazepine structure was identified as lead structure in a diverse series of 3-amino-1,4-benzodiazepines 4-38 and the full SAR (structure-activity relationship) optimisation provided 3-anilinobenzodiazepines 16-38 with CCK 1 receptor selectivity to CCK 2. The compounds 18, 24, 28 and 33 have shown affinities at the CCK 1 receptor of 11, 10, 11 and 9 nM, respectively. These equipotent CCK 1 ligands were fully evaluated in behaviour pharmacological essays. An antidepressant effect was identified in the tail suspension- and the Porsolt swimming-test. The ED 50 values for 24 and 28 were determined in these assays as 0.46 and 0.49 mg/kg. The mixed antagonist 37 showed in addition to the antidepressant effects anxiolytic properties. © 2006 Wiley-VCH Verlag GmbH & Co. KGaA.

Intelligent Computations for Flood Monitoring

Floods represent the most devastating natural hazards in the world, affecting more people and causing more property damage than any other natural phenomena. One of the important problems associated with flood monitoring is flood extent extraction from satellite imagery, since it is impractical to acquire the flood area through field observations. This paper presents a method to flood extent extraction from synthetic-aperture radar (SAR) images that is based on intelligent computations. In particular, we apply artificial neural networks, self-organizing Kohonen’s maps (SOMs), for SAR image segmentation and classification. We tested our approach to process data from three different satellite sensors: ERS-2/SAR (during flooding on Tisza river, Ukraine and Hungary, 2001), ENVISAT/ASAR WSM (Wide Swath Mode) and RADARSAT-1 (during flooding on Huaihe river, China, 2007). Obtained results showed the efficiency of our approach.

Efficient asynchronous scheduling algorithms for cost-effective buffered crossbar switches

Buffered crossbar switches have recently attracted considerable attention as the next generation of high speed interconnects. They are a special type of crossbar switches with an exclusive buffer at each crosspoint of the crossbar. They demonstrate unique advantages over traditional unbuffered crossbar switches, such as high throughput, low latency, and asynchronous packet scheduling. However, since crosspoint buffers are expensive on-chip memories, it is desired that each crosspoint has only a small buffer. This dissertation proposes a series of practical algorithms and techniques for efficient packet scheduling for buffered crossbar switches. To reduce the hardware cost of such switches and make them scalable, we considered partially buffered crossbars, whose crosspoint buffers can be of an arbitrarily small size. Firstly, we introduced a hybrid scheme called Packet-mode Asynchronous Scheduling Algorithm (PASA) to schedule best effort traffic. PASA combines the features of both distributed and centralized scheduling algorithms and can directly handle variable length packets without Segmentation And Reassembly (SAR). We showed by theoretical analysis that it achieves 100% throughput for any admissible traffic in a crossbar with a speedup of two. Moreover, outputs in PASA have a large probability to avoid the more time-consuming centralized scheduling process, and thus make fast scheduling decisions. Secondly, we proposed the Fair Asynchronous Segment Scheduling (FASS) algorithm to handle guaranteed performance traffic with explicit flow rates. FASS reduces the crosspoint buffer size by dividing packets into shorter segments before transmission. It also provides tight constant performance guarantees by emulating the ideal Generalized Processor Sharing (GPS) model. Furthermore, FASS requires no speedup for the crossbar, lowering the hardware cost and improving the switch capacity. Thirdly, we presented a bandwidth allocation scheme called Queue Length Proportional (QLP) to apply FASS to best effort traffic. QLP dynamically obtains a feasible bandwidth allocation matrix based on the queue length information, and thus assists the crossbar switch to be more work-conserving. The feasibility and stability of QLP were proved, no matter whether the traffic distribution is uniform or non-uniform. Hence, based on bandwidth allocation of QLP, FASS can also achieve 100% throughput for best effort traffic in a crossbar without speedup.

Evaluation of TerraSAR-X Observations for Wetland InSAR Application

This paper assesses the potential of using spaceborne X-band synthetic aperture radar (SAR) data for monitoring water-level changes over wetlands. Our analysis is based on three sets of TerraSAR-X (TSX) observations acquired over South Florida's Everglades wetlands during an eight-month period in 2008. The first set was acquired in single HH polarization stripmap mode over our northern study area, consisting of managed wetlands and urban environments. The second set was acquired in dual-polarization stripmap mode over the western half of the same area, consisting mostly of managed wetlands. The third set was also acquired with dual-polarization stripmap mode over our southern study area, consisting of natural flow freshand salt-water wetlands in the southern Everglades. The first data set was used for a proof-of-concept study to verify that X-band data can generate coherent interferograms in wetland areas. Interferometric processing of this data set shows a high level of coherence (> 0.35) over both wetland and urban regions, maintaining interferometric phase in all three interferograms spanning 11 days. Surprisingly, phase is maintained over some of the wetlands even for interferograms spanning 33 days. The other two data sets were used to evaluate interferometric coherence of all four polarization modes and to determine dominant scattering mechanism in each wetland environment. Our results show high coherence values (> 0.4) in all polarization modes, with highest values in HH, then VV, and lowest in HV or VH. Interferograms calculated from multipolarization data show very similar fringe patterns regardless of the polarization type, suggesting that the phase information in all polarization data reflects water-level changes in wetlands and that volume scattering may be less important than commonly believed. We also used the two multipolarization data sets to conduct the Pauli decomposition, finding a strong dependence of scattering mechanism on vegetation t- - ype. The high interferometric coherence level of all polarization data suggests that a significant part of the X-band scattered signal interacts with lower sections of the vegetation (trunks and branches), because scattering from wind-affected canopies cannot support such a high coherence level. The high spatial resolution of TSX, combined with its 11-day repeat orbit, makes this X-band sensor surprisingly suitable for wetland interferometric SAR applications.

Host and network optimizations for performance enhancement and energy efficiency in data center networks

Modern data centers host hundreds of thousands of servers to achieve economies of scale. Such a huge number of servers create challenges for the data center network (DCN) to provide proportionally large bandwidth. In addition, the deployment of virtual machines (VMs) in data centers raises the requirements for efficient resource allocation and find-grained resource sharing. Further, the large number of servers and switches in the data center consume significant amounts of energy. Even though servers become more energy efficient with various energy saving techniques, DCN still accounts for 20% to 50% of the energy consumed by the entire data center. The objective of this dissertation is to enhance DCN performance as well as its energy efficiency by conducting optimizations on both host and network sides. First, as the DCN demands huge bisection bandwidth to interconnect all the servers, we propose a parallel packet switch (PPS) architecture that directly processes variable length packets without segmentation-and-reassembly (SAR). The proposed PPS achieves large bandwidth by combining switching capacities of multiple fabrics, and it further improves the switch throughput by avoiding padding bits in SAR. Second, since certain resource demands of the VM are bursty and demonstrate stochastic nature, to satisfy both deterministic and stochastic demands in VM placement, we propose the Max-Min Multidimensional Stochastic Bin Packing (M3SBP) algorithm. M3SBP calculates an equivalent deterministic value for the stochastic demands, and maximizes the minimum resource utilization ratio of each server. Third, to provide necessary traffic isolation for VMs that share the same physical network adapter, we propose the Flow-level Bandwidth Provisioning (FBP) algorithm. By reducing the flow scheduling problem to multiple stages of packet queuing problems, FBP guarantees the provisioned bandwidth and delay performance for each flow. Finally, while DCNs are typically provisioned with full bisection bandwidth, DCN traffic demonstrates fluctuating patterns, we propose a joint host-network optimization scheme to enhance the energy efficiency of DCNs during off-peak traffic hours. The proposed scheme utilizes a unified representation method that converts the VM placement problem to a routing problem and employs depth-first and best-fit search to find efficient paths for flows.

Understanding Annual Reports of Hospitality Firms: Part II

This is the second article in a two-part series on understanding annual reports published by publicly-held hospitality firms. Part I in the Spring 1988 issue established the informational content of such reports while this article will focus on the examination and understanding of annual reports, suggested guidelines on how to use them for decision making, and recent developments affecting these reports.

Helicopter-borne sea ice thickness measurements in the Storfjord, Spitsbergen from flight HEM_STJ06_01

Results from electromagnetic induction surveys of sea-ice thickness in Storfjorden, Svalbard, reveal large interannual ice-thickness variations in a region which is typically characterized by a reoccurring polynya. The surveys were performed in March 2003, May 2006 and March 2007 with helicopter- and ship-based sensors. The thickness distributions are influenced by sea-ice and atmospheric boundary conditions 2 months prior to the surveys, which are assessed with synthetic aperture radar (SAR) images, regional QuikSCAT backscatter maps and wind information from the European Centre for Medium-Range Weather Forecasts (ECMWF) reanalysis dataset. Locally formed thin ice from the Storfjorden polynya was frequently observed in 2003 and 2007 (mean thickness 0.55 and 0.37 m, respectively) because these years were characterized by prevailing northeasterly winds. In contrast, the entire fjord was covered with thick external sea ice in 2006 (mean thickness 2.21 m), when ice from the Barents Sea was driven into the fjord by predominantly southerly winds. The modal thickness of this external ice in 2006 increased from 1.2 m in the northern fjord to 2.4 m in the southern fjord, indicating stronger deformation in the southern part. This dynamically thickened ice was even thicker than multi-year ice advected from the central Arctic Ocean in 2003 (mean thickness 1.83 m). The thermodynamic ice thickness of fast ice as boundary condition is investigated with a one-dimensional sea-ice growth model (1DICE) forced with meteorological data from the weather station at the island of Hopen, southeast of Storfjorden. The model results are in good agreement with the modal thicknesses of fast-ice measurements in all years.

Strategie di intervento per la difesa del mare e della costa dagli inquinamenti accidentali di idrocarburi

Il presente lavoro di tesi nasce dall’esigenza di comprendere e studiare come viene affrontata, e gestita, l’emergenza in mare derivante dallo sversamento accidentale, o volontario, di idrocarburi; il sistema di risposta nazionale a questo genere di emergenze si sviluppa su più livelli e per ogni livello sono individuati gli organi responsabili e i relativi compiti. Le azioni da intraprendere sono specificate negli elaborati di pianificazione redatti dall’Agenzia Nazionale di Protezione Civile, dal Ministero dell’Ambiente e della Tutela del territorio e del Mare, dalle Capitanerie di Porto Locali, dalle Province e dai Comuni; i primi 3 si occupano dell’emergenza in mare, mentre le Province e i Comuni si occupano degli interventi da attuare sulla costa in seguito allo spiaggiamento degli idrocarburi. La regione Emilia-Romagna, in particolare, non possiede elaborati di pianificazione per la gestione del rischio di inquinamento costiero; per questo motivo, sulla base delle indicazioni riportate negli elaborati di pianificazione nazionale e consultando elaborati già esistenti di altre regioni adriatiche, è stata redatta una proposta di linee guida per la redazione di un Piano Comunale d’Emergenza che preveda il rischio di inquinamento costiero. Per poter prevedere quale tecnica di bonifica sarà possibile applicare ad uno sversamento di idrocarburi, esistono software che modellano i processi chimico-fisici che la sostanza subisce con il passare del tempo. Ogni tecnica ha dei limiti sia di efficienza che di applicabilità; essi sono principalmente dovuti alle condizioni meteomarine e ai processi che la sostanza subisce nel tempo una volta sversata; la conoscenza di questi limiti permette di effettuare, nella maggior parte delle situazioni, la scelta della tecnica di intervento più appropriata ed efficiente a seconda della situazione. La tesi è strutturata come segue. Nel Capitolo 1 sono descritte le problematiche e le cause relative agli incidenti in mare che comportano il rilascio di idrocarburi in esso e gli effetti che questi hanno sull’ambiente e i cambiamenti che la sostanza subisce una volta sversata in mare. Nel Capitolo 2 sono descritte le strategie di intervento per il recupero degli idrocarburi sversati in mare e le tecniche di bonifica attuabili sulla costa impattata dallo sversamento. Nel Capitolo 3 è illustrato il sistema di risposta nazionale all’emergenza derivante dallo sversamento in mare di idrocarburi; ad ogni livello è dedicato un paragrafo del Capitolo 3. Inoltre sono presentate delle linee guida per la redazione di un Piano Comunale d’Emergenza che preveda il Rischio di Inquinamento Costiero da idrocarburi e altre sostanza nocive. Nel Capitolo 4 è illustrato il software ADIOS 2 che permette di modellare i processi chimico-fisici che la sostanza subisce quando viene sversata in mare e di simulare l’utilizzo di alcune strategie di intervento. Nel Capitolo 5 sono riportate le considerazioni conclusive e i risultati ottenuti.

Petrographic and geochemical characterization of a sample taken from the beni bousera peridotite (Morocco)

Il massiccio di Beni Bousera (Marocco) è formato da diverse unità geologiche composte prevalentemente da rocce metamorfiche molto simili a quelle che si trovano nel massiccio di Ronda (Spagna). Queste due catene montuose erano connesse prima dell’estensione (iniziata nel Miocene inferiore) che le ha separate lasciando il posto al mare di Alborán. Questo studio sarà incentrato soltanto sul massiccio marocchino, in particolare sull’unità peridotitica di Beni Bousera. Questa unità è stata suddivisa in quattro domini, ognuno dei quali ha specifiche caratteristiche petrologiche e geochimiche, che sono il risultato di diverse condizioni metamorfiche e di diversi regimi tettonici. L’obiettivo di questo lavoro è di caratterizzare, dal punto di vista petrologico, un campione che è stato prelevato dal massiccio di Beni Bousera, nella zona costiera del mare di Alborán e di determinare a quale dominio esso appartiene.

Definizione e validazione di uno strumento per la misurazione dell'impatto delle variabili redazionali di un item matematico sulla performance degli studenti

Questa tesi descrive la ricerca condotta tra l'autunno e l'inverno di quest'anno da un gruppo di ricercatori in didattica della matematica relativamente all'influenza che le variazioni redazionali di un quesito matematico hanno sulle performance degli studenti. Lo scopo della ricerca è quella di strutturare e validare una metodologia e uno strumento che permettano di individuare e quantificare l'influenza delle variazioni del testo sulle prestazioni dello studente. Si è sentita l'esigenza di condurre uno studio di questo tipo poichè è sempre più evidente il profondo legame tra il linguaggio e l'apprendimento della matematica. La messa a punto di questo strumento aprirebbe le porte a una serie di ricerche più approfondite sulle varie tipologie di variazioni numeriche e/o linguistiche finora individuate. Nel primo capitolo è presentato il quadro teorico di riferimento relativo agli studi condotti fino ad ora nell'ambito della didattica della matematica, dai quali emerge la grossa influenza che la componente linguistica ha sulla comprensione e la trasmissione della matematica. Si farà quindi riferimento alle ricerche passate volte all'individuazione e alla schematizzazione delle variazioni redazionali dei Word Problems. Nel secondo capitolo, invece si passerà alla descrizione teorica relativa allo strumento statistico utilizzato. Si tratta del modello di Rasch appartenente alla famiglia dei modelli statistici dell'Item Response Theory, particolarmente utilizzato nella ricerca in didattica. Il terzo capitolo sarà dedicato alla descrizione dettagliata della sperimentazione svolta. Il quarto capitolo sarà il cuore di questa tesi; in esso infatti verrà descritta e validata la nuova metodologia utilizzata. Nel quinto sarà eseguita un analisi puntuale di come lo strumento ha messo in evidenza le differenze per ogni item variato. Infine verranno tratte le conclusioni complessive dello studio condotto.