322 research outputs found
A NASA/RAE cooperation in the development of a real-time knowledge-based autopilot
As part of a US/UK cooperative aeronautical research program, a joint activity between the NASA Dryden Flight Research Facility and the Royal Aerospace Establishment on knowledge-based systems was established. This joint activity is concerned with tools and techniques for the implementation and validation of real-time knowledge-based systems. The proposed next stage of this research is described, in which some of the problems of implementing and validating a knowledge-based autopilot for a generic high-performance aircraft are investigated
Determination of the Primary Molecular Target of 1,2,4-Triazole-Ciprofloxacin Hybrids
We have synthesized and examined the antibacterial activity, toxicity and
affinity towards bacterial type II topoisomerases of a series of 1,2,4-triazole-ciprofloxacin
hybrids. A number of these compounds displayed enhanced activity against Gram-positive
and Gram-negative bacteria when compared to ciprofloxacin. The toxic concentrations of
the obtained derivatives, evaluated on HEK-293 cells using MTT assay, were much higher
than concentrations required to produce antibacterial effect. Finally, the results of
enzymatic studies showed that the analyzed compounds demonstrated other preferences as
regards primary and secondary molecular targets than ciprofloxacin.This research was supported by the Ministry of Science and Higher Education under Iuventus Plus
grant No. IP2014 037473. Tomasz Plech is a recipient of the Fellowship for Young Researchers with
Outstanding Scientific Achievements from the Medical University of Lublin (Lublin, Poland)
Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies
The combination of antagonism at histamine H3 receptor and the stimulation of insulin secretion have been proposed as an approach to new dual therapeutic agents for the treatment of type 2 diabetes mellitus associated with obesity. We have designed and synthesized a new series of non-imidazole derivatives, based on a basic amine ring connected through an alkyl spacer of variable length to a phenoxysulfonylurea moiety. These compounds were initially evaluated for histamine H3 receptor binding affinities, suggesting that a propoxy chain linker between the amine and the core ring could be essential for optimal binding affinity. Compound 56, 1-(naphthalen-1-yl)-3-[(p-(3-pyrrolidin-1-ylpropoxy)benzene)]sulfonylurea exhibited the best H3 antagonism affinity. However, since all these derivatives failed to block KATP channels, the link of these two related moieties should not be considered a good pharmacophore for obtaining new dual H3 antagonists with insulinotropic activity, suggesting the necessity to propose a new chemical hybrid prototype
Legislative History: An Act to Amend the Motor Vehicle Laws (SP753)(LD 2031)
https://digitalmaine.com/legishist118/3030/thumbnail.jp
Legislative History: An Act to Amend the Charter of the Sanford Sewerage District (SP709)(LD 1957)
https://digitalmaine.com/legishist118/2956/thumbnail.jp
Legislative History: An Act to Restore Advocacy for Handicapped Students (HP1521)(LD 2143)
https://digitalmaine.com/legishist118/3142/thumbnail.jp
Legislative History: An Act to Address the Crisis in Access to Dental Care for Low-income Children (HP1515)(LD 2137)
https://digitalmaine.com/legishist118/3136/thumbnail.jp
Legislative History: An Act to Promote Safety of Families through the Workplace (HP1463)(LD 1960)
https://digitalmaine.com/legishist120/2959/thumbnail.jp
Legislative History: Joint Order to Recall LD 1923 from the Governor\u27s Desk to the House (HP1729)
https://digitalmaine.com/legishist120/3396/thumbnail.jp
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