A Catalytic One-Pot Synthesis of Indolyl Cyclobutanones

A general strategy for the synthesis of indolyl cyclobutanones via a tandem Bronsted acid catalyzed 2-hydroxycyclobutanone activation-indole nucleophilic addition has been exploited. The procedure leads to a wide range of 2- and 3-functionalized indole derivatives in good to high yields with broad substrate scope

Dynamic cloudlet assignment problem: A column generation approach

Major interest in network optimization is currently given to the integration of clusters of virtualization servers, also referred to as 'cloudlets', into mobile access networks for improved performance and reliability. Mobile access points (APs) are assigned (i.e., route their packets) to one or more cloudlets, with a cost in terms of latency for the users they provide connections to. Assignment of APs to cloudlet can be changed over time, with a cloudlet synchronization cost. We tackle the problem of the optimal assignment of APs to cloudlets over time, proposing dedicated mathematical models and column generation algorithms

Design, synthesis and biological activity of selective hCAs inhibitors based on 2-(benzylsulfinyl)benzoic acid scaffold

A large library of derivatives based on the scaffold of 2-(benzylsulfinyl)benzoic acid were synthesised and tested as atypical inhibitors against four different isoforms of human carbonic anhydrase (hCA I, II, IX and XII, EC 4.2.1.1). The exploration of the chemical space around the main functional groups led to the discovery of selective hCA IX inhibitors in the micromolar/nanomolar range, thus establishing robust structure-activity relationships within this versatile scaffold. HPLC separation of some selected chiral compounds and biological evaluation of the corresponding enantiomers was performed along with molecular modelling studies on the most active derivatives

Asymmetric Organocatalysis-A Powerful Technology Platform for Academia and Industry: Pregabalin as a Case Study

Enantioselective organocatalysis has quickly established itself as the third pillar of asymmetric catalysis. It is a powerful technology platform, and it has a tremendous impact in both academic and industrial settings. By focusing on pregabalin, as a case study, this Perspective aims to show how a process amenable to industry of a simple chiral molecule can be tackled in several different ways using organocatalysis

Mobile Edge Cloud Network Design Optimization

Major interest is currently given to the integration of clusters of virtualization servers, also referred to as 'cloudlets' or 'edge clouds', into the access network to allow higher performance and reliability in the access to mobile edge computing services. We tackle the edge cloud network design problem for mobile access networks. The model is such that the virtual machines (VMs) are associated with mobile users and are allocated to cloudlets. Designing an edge cloud network implies first determining where to install cloudlet facilities among the available sites, then assigning sets of access points, such as base stations to cloudlets, while supporting VM orchestration and considering partial user mobility information, as well as the satisfaction of service-level agreements. We present link-path formulations supported by heuristics to compute solutions in reasonable time. We qualify the advantage in considering mobility for both users and VMs as up to 20% less users not satisfied in their SLA with a little increase of opened facilities. We compare two VM mobility modes, bulk and live migration, as a function of mobile cloud service requirements, determining that a high preference should be given to live migration, while bulk migrations seem to be a feasible alternative on delay-stringent tiny-disk services, such as augmented reality support, and only with further relaxation on network constraints

Solvent-Free Synthesis of Quaternary Oxazolidine-2-thione β3-Amino Ester Analogs

A solvent-free organocatalyzed intermolecular cyclization reaction starting from β-substituted γ-hydroxy-α,β-unsaturated esters and aryl isothiocyanates proceeds via an aza-Michael addition to provide previously unknown quaternary oxazolidine-2-thione β3 amino ester analogs. A panel of diversely-substituted esters was investigated, including β,γ-disubstituted examples which provided the target molecules with very high cis diastereoselectivity

Study of Packaging and Installation of FBG Sensors for Monitoring of Aircraft Systems

Next generation aircraft systems will feature an ever increasing complexity. In this context, advanced health monitoring strategies will be required to ensure a high level of operations safety as well as a good reliability. Hence, Prognostics and Health Management (PHM) is emerging as an enabling discipline for future advanced aircraft design and operations, with a particular application to Flight Control System (FCS) monitoring. One of the most critical issues for real-time Fault Detection and Identification (FDI) of aircraft FCS is the availability of actuator load measurements. The aerodynamic load on flight control actuators has a significant influence on their dynamic response, and can easily hide the effect of incipient failure precursors. For this reason, real-time monitoring FDI algorithms relying on the comparison between the actual system response and that of a digital twin require either a measure or an estimation of aerodynamic loads. Usually, this quantity is not monitored by a dedicated sensor, since it is not required as a feedback signal by most control logics. A dedicated load sensor for PHM with traditional technologies is not easily feasible: for example, a load cell would be mechanically connected in series with the actuator, adding a potential single failure point and affecting the overall system safety; the use of strain gages on the structure is less accurate, and requires several sensors with individual wiring and complex signal conditioning circuitry. Optical strain sensors based on Fiber Bragg Gratings (FBG) allow indirect load measurement combined with real-time structural monitoring, combining an acceptable increase in complexity and costs with a high robustness. In this preliminary study, we installed an FBG monitoring system on a UAV to assess the feasibility of such technology. Measures of structure deflection were correlated to actuator position and IMU data, to estimate aerodynamic loads

Novel insights on saccharin- and acesulfame-based carbonic anhydrase inhibitors: design, synthesis, modelling investigations and biological activity evaluation

A large library of saccharin and acesulfame derivatives has been synthesised and evaluated against four isoforms of human carbonic anhydrase, the two off-targets hCA I/II and the tumour related isoforms hCA IX/XII. Different strategies of scaffold modification have been attempted on both saccharin as well as acesulfame core leading to the obtainment of 60 compounds. Some of them exhibited inhibitory activity in the nanomolar range, albeit some of the performed changes led to either micromolar activity or to its absence, against hCA IX/XII. Molecular modelling studies focused the attention on the binding mode of these compounds to the enzyme. The proposed inhibition mechanism is the anchoring to zinc-bound water molecule. Docking studies along with molecular dynamics also underlined the importance of the compounds flexibility (e.g. achieved through the insertion of methylene group) which favoured potent and selective hCA inhibition