Discovery of Broad-Spectrum Herpes Antiviral Oxazolidinone Amide Derivatives and Their Structure–Activity Relationships
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Engineering topics
Publications and source records attributed to Berger, Richard.
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Abstract not provided
In this paper we describe the development of a series of pyrazolopyrimidinone phosphodiesterase 2A (PDE2) inhibitors using structure-guided lead identification and design. The series was derived from informed chemotype replacement based on previously identified internal leads. The initially designed compound 3, while potent on PDE2, displayed unsatisfactory selectivity against the other PDE2 isoforms. Compound 3 was subsequently optimized for improved PDE2 activity and isoform selectivity. Insights into the origins of PDE2 selectivity are described and verified using cocrystallography. An optimized lead, 4, demonstrated improved performance in both a rodent and a nonhuman primate cognition model.
LOKI is a simulation code that models weakly-coupled plasma evolution using Eulerian kinetic models in four phase space dimensions. The code is useful to understand basic plasma nonlinear plasma physics phenomena - in particular, wave-particle and wave-wave resonances that occur in laser plasma interactions. LOKI can simulate fundamental physical process in low-density plasmas on a scale of hundreds of light wavelengths. It does so by solving the Vlasov and Valsov-Fokker-Planck differential transport equations describing the collision less and low-collisionality evolution of charged particles in electromagnetic fields in two configuration space and two velocity space dimensions. Two principle electromagnetic models are provided: electrostatic (Poisson's Equation) and electromagnetic (Maxwell's equations).
An Application Specific Integrated Circuit (ASIC) that implements the SpaceWire protocol has been developed in a radiation hardened 0.25 micron CMOS, technology. This effort began in March 2003 as a joint development between the NASA Goddard Space Flight Center (GSFC) and BAE Systems. The BAE Systems SpaceWire ASlC is comprised entirely of reusable core elements, many of which are already flight-proven. It incorporates a 4-port SpaceWire router with two local ports, dual PC1 bus interfaces, a microcontroller, 32KB of internal memory, -and a memory controller for additional external memory use. The SpaceWire ASlC is planned for use on both the Geostationary Operational Environmental Satellites (GOES)-R and the Lunar Reconnaissance Orbiter (LRO). Engineering parts have already been delivered to both programs. This paper discusses the SpaceWire protocol and those elements of it that have been built into the current SpaceWire reusable core. There are features within the core that go beyond the current standard that can be enabled or disabled by the user and these will be described. The adaptation of SpaceWire to BAE Systems' On Chip Bus (OCB) for compatibility with the other reusable cores will be discussed. Optional configurations within user systems will be shown. The physical imp!ementation of the design will be described and test results from the hardware will be discussed. Finally, the BAE Systems roadmap for SpaceWire developments will be discussed, including some products already in design as well as longer term plans.