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  • 44 Reads
Automation in Reaction Optimization
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The use of automation in high-throughput screening and high-speed parallel synthesis has been well documented in recent years1. While combinatorial techniques and automation are beginning to permeate material science and catalyst research2, the benefits of automation in reaction development is a largely untapped. Our approach towards automating reaction optimization is based on the utilization of a robotics lab designed to accommodate a wide range of applications. This is achieved through the principle of unit operations. Unit operations can be described as basic tasks that are performed normally in chemistry such as the manipulation of liquids and the weighing of starting materials. This approach is based on using a number of workstations that can achieve the automation of these tasks and accelerate a given operation. Automated workstations are designed to carry out a small number of tasks very well. They are most useful when employed as specialized instruments. When they are built to perform complex processes, problems often arise.
  • Open access
  • 47 Reads
LQ12, A Novel PKC Activator, Enhances sAPP Secretion in PC-12 Cells
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Research on cellular and molecular aspects of Alzheimer’s disease over the last two decades has resulted in a significantly improved understanding of this disease. Particular achievements have occurred in the areas of molecular genetics and the biology of amyloid. This research has strengthened the notion that Ab is a central player in the disease process.1-5 Despite the progress and the data accumulated, the understanding of the pathophysiological framework remains incipient. Consequently, rational drug design targeting specific pathophysiological events or chemical entities has seen little or slow progress. Additional difficulties arise from the fact that dynamic processes are difficult to assess in the AD brain as a number of signal transduction mechanisms are altered by postmortem events.6 In addition, AD brain tissue usually becomes available after a long period of the disease, at an advanced pathological state. Therefore, significant effort has been devoted to alternative approaches.6-10 A host of cellular and molecular changes ranging from nucleic acid defects to second messenger alterations have been described in peripheral cells of AD patients.6-8,10,11 Some alterations have also been observed in neuronal animal cells and brain.12-15 Of the many alterations, PKC seems uniquely situated in the cascade of events (normal and pathological) interacting with Ab, calcium homeostasis and ion channel function. Herein we propose a framework as an initial step for drug design targeting PKC
  • Open access
  • 45 Reads
A Novel Synthesis of Porphobilinogen: Synthetic and Biosynthetic Studies.
Importance of the "pigments of life" The studies of the tetrapyrrolic dyes, which have been called the "pigments of life"[1] have attracted the attention of chemists and biologists since their discovery. The importance of the "pigments of life" as crucial cofactors for processes like photosynthesis, oxygen transport, oxidation processes, methane synthesis and for a series of unusual rearrangements illustrates well the central role played by this class of natural products.
  • Open access
  • 57 Reads
Synthesis of N,N'-diarylalkanediamides and their antimycobacterial and antialgal activity
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A set of N,N'-diarylalkanediamides was synthesised. The compounds were tested for their antimycobacterial and antialgal activity. The antimycobacterial activity of N,N'-diarylalkanediamides depends on the lipophilicity of the respective acid. Antimycobacterially active substances were found only in the series of N,N'-diarylethanediamides and N,N'-diarylbutanediamides. Other compounds (derivatives of pentane-, hexane-, octane- and nonanediamide) were inactive against various strains of mycobacteria. The compounds inhibited growth and chlorophyll production in Chlorella vulgaris. Their relatively low antialgal activity is caused by their low aqueous solubility, and hence by a restricted passage of the inhibitor through the hydrophilic regions of thylakoid membranes.
  • Open access
  • 57 Reads
Synthesis of some anilides of 2-alkylsulfanyl- and 2-chloro-6-alkylsulfanyl-4-pyridinecarboxylic acids and their photosynthesis-inhibiting activity
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A group of anilides of 2-alkylsulfanyl- (I) or 2-chloro-6-alkylsulfanyl-4-pyridinecarboxylic acids (II) was synthesised. The prepared compounds were tested for inhibition of photosynthesis upon oxygen evolution rate in spinach chloroplasts. The IC50 values varied in the range of 6.0--69.1 μmol.dm-3 for I and 14.2--32.5 μmol.dm-3 for II. The inhibitory activity of I and II showed a quasi-parabolic dependence upon the lipophilicity (log P) of the compounds. For compounds with comparable lipophilicity the presence of chloro substituent in position 2 of the pyridine moiety led to the decrease of inhibitory activity.
  • Open access
  • 52 Reads
Steroidal Tetraoxanes - New Class of Antitumor Compounds
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Cholic acid derived steroidal tetraoxanes possessing methyl ester, carboxylic acid, primary and secondary amide termini were synthesised and their in vitro antitumor activity against Fem-X and HeLa cell cultures was determined. IC50 range between 3.1 and 166 M. Five out of seven tested compounds exhibited cell rounding and / or apoptic activity. Their liquid secondary ionization (LSI) and electronspray ionization (ESI) spectra confirmed the tetraoxane structure.
  • Open access
  • 44 Reads
A small company perspective on partnering with large pharma.
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The nature of the start-up company in the bio-tech or bio-pharma field is complex and constantly evolving. At the heart of the company is the desire of its founders to bring to fruition their concepts and dreams in an economically successful frame work. The objectives are to efficiently utilize capital to advance the concepts (which quickly become technologies) through a series of stages that will prove feasibility and add value. In drug industry terms start-ups want to move their intellectual property from concept to feasibility through models of efficacy and safety. At each stage success brings added value, all things being equal. The forces acting upon the company are manifold. Success of candidate molecules is never assured, competition is intense and the process itself is expensive. In addition, investors seek good returns on their invested capital, which translate into an exit strategy that will generate liquid assets.
  • Open access
  • 39 Reads
Cold plasma induced chemical reactions. Implications for molecular evolution
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The main aspects of the chemical origins of life research concern the synthesis of so called prebiotic compounds, such as amino acids, purine and pirimidine bases, sugars, etc., and the subsequent steps of their condensation up to proteins and nucleic acids. However, most studies are frequently dedicated to the synthesis of individual compounds, ignoring the complexity of the medium in which they evolved. Cold plasma laboratory simulations corroborated with thermodynamic calculations and space observations are presented.
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