Synthesis and Preliminary Biological Evaluation of 1,3,5-Triazine Amino Acid Derivatives to Study Their MAO Inhibitors
Three series of 4,6-dimethoxy-, 4,6-dipiperidino- and 4,6-dimorpholino-1,3,5-triazin-2-yl) amino acid derivatives were synthesized and characterized. A preliminary study for their monoamine oxidase inhibitory activity showed that compounds 7, 18, and 25 had MAO-A inhibition activity comparable to that of the standard clorgyline, with apparently more selective inhibitory activity toward MAO-A than MAO-B and no significant acute toxicity.
Design and synthesis of a novel family of triazine-based inhibitors of sorbitol dehydrogenase with oral activity: 1-[4-[3R,5S-dimethyl-4-(4-methyl-[1,3,5]triazin-2-yl)-piperazin-1-yl]-[1,3,5]triazin-2-yl]-(R) ethanol.
Two new templates, (R) 2-hydroxyethyl-pyridine and (R) 2-hydroxyethyl-triazine, were used to design novel sorbitol dehydrogenase inhibitors (SDIs). The design concept included spawning of these templates to function as effective ligands to the catalytic zinc within the enzyme through incorporation of optimally substituted piperazino-triazine side chains so as to accommodate the active site in the enzyme for efficient binding. This strategy resulted in orally active SDIs, which penetrate key tissues, for example, sciatic nerve of chronically diabetic rats. The latter template led to the design of the title inhibitor, 33, which normalized the elevated sciatic nerve fructose by 96% at an oral dose of 10mg/kg.
Interviewing In Context
PART ONE: PRELIMINARY CONSIDERATIONS. An Introduction to Interviewing. Understanding Contextual Factors. PART TWO: BASIC CONSIDERATIONS: FOUNDATIONS FOR COMMUNICATION. Developing the Structure of the Interview. Understanding Questions. Using Questions. PART THREE: ORGANIZATIONAL CONTEXTS. The Selection Interview: The Interviewer's Perspective. The Selection Interview: The Applicant's Perspective. The Performance Appraisal Interview. PART FOUR: PROFESSIONAL CONTEXTS. The In-Depth Information Gathering Interview. The Survey Interview. The Problem-Solving Interview. The Persuasive Interview