High Throughput Technology in Compound Synthesis

To test a vast number of compounds for biological activity

Freezing the equilibrium reactions and performing an irreversible reaction to convert all equilibrium products to stable compounds

Mostly optical assays (fluorescence, luminescence, absorbance)

<p>Significant cost savings and less sample per assay</p> Signup and view all the answers

<p>Acting as the target for the reaction</p> Signup and view all the answers

<p>Generates more of the active compound (Amplification!)</p> Signup and view all the answers

<p>To synthesize and detect specific products on a plate with high resolution.</p> Signup and view all the answers

<p>Safety Catch ensures the target molecule is safe on the linker until a specific step is performed, while acid-labile linker releases the target molecule with an acid treatment.</p> Signup and view all the answers

<p>In DCS, all compounds are synthesized simultaneously in one flask and screened as they are formed, whereas mix and split synthesis involves sequential steps.</p> Signup and view all the answers

<p>The group is used for deprotection of specific sites on the solid support, allowing coupling with protected amino acids.</p> Signup and view all the answers

<p>Peptide microsequencing helps determine the code attached to the Lys residue on beads, allowing identification of synthesized peptides.</p> Signup and view all the answers

<p>Different masks expose specific areas on the plate for deprotection, leading to the synthesis of peptide chains with varied sequences.</p> Signup and view all the answers

<p>Combinatorial synthesis (CS) and Parallel synthesis (PS)</p> Signup and view all the answers

<p>Easier to identify the synthesized structures in PS.</p> Signup and view all the answers

<p>Generation of many more structures compared to PS.</p> Signup and view all the answers

<p>Merrifield resin peptide synthesis</p> Signup and view all the answers

<p>Polystyrene is too hydrophobic, leading to peptide chain folding in on itself.</p> Signup and view all the answers

<p>Wang and Rink resins</p> Signup and view all the answers

<p>Peptides</p> Signup and view all the answers

<p>GABAA receptors modulation</p> Signup and view all the answers

<p>To achieve structural diversity by having a central body and arms bearing different functional groups.</p> Signup and view all the answers

<p>Higher success rates for finding leads due to better exploration of 3D space around the molecule.</p> Signup and view all the answers

<p>Ugi, Biginelli, Passerini reaction</p> Signup and view all the answers

<p>F-SPE uses highly fluorinated silica to remove fluorinated compounds, while basic column extraction removes acidic impurities.</p> Signup and view all the answers

<p>Scavenger resins are used to eliminate excess reagent and yield pure product.</p> Signup and view all the answers

<p>Catch-and-Release involves attaching a reagent to a resin, which can be easily removed by filtration after the reaction is completed.</p> Signup and view all the answers

<p>Carboxylic acid, coupling reagent (resin-bound), and existing questions.</p> Signup and view all the answers

<p>Excess amine is consumed by adding fluorinated isocyanate after the reaction, and then the fluorinated urea derivative is removed by F-SPE.</p> Signup and view all the answers

<p>Shorter reaction times, fewer by-products, higher yield, good control of temperature, potential for a vast number of chemical reactions on one chip</p> Signup and view all the answers

<p>It is a method that allows for the generation of multiple compounds by mixing and then splitting them, saving time compared to individual syntheses.</p> Signup and view all the answers

<p>To generate large amounts of compounds quickly for testing biological activity as mixtures.</p> Signup and view all the answers

<p>MAOS accelerates synthesis using microwaves, resulting in higher efficiency and often greener processes.</p> Signup and view all the answers

<p>It enables the synthesis of compounds from multiple building blocks simultaneously, reducing the time and effort required.</p> Signup and view all the answers

<p>It allows for the generation of the dipeptide in less time by combining and splitting the building blocks efficiently.</p> Signup and view all the answers

<p>To help with structural identification by tagging/coding compounds</p> Signup and view all the answers

<p>Tags are used to code each synthetic step, allowing for the identification of the specific sequence of the final compound.</p> Signup and view all the answers

<p>In two steps: one involving the cleavage of the tag, followed by the release of the target molecule.</p> Signup and view all the answers

<p>It allows for the structural identification of compounds in a mixture by utilizing tagging/coding techniques.</p> Signup and view all the answers

<p>Each tag corresponds to a specific synthetic step in the synthesis process.</p> Signup and view all the answers

<p>It facilitates both the synthesis of target molecules and the coding of compounds, aiding in structural identification.</p> Signup and view all the answers

<p>To determine the code attached to the bead</p> Signup and view all the answers

<p>By exposing specific parts of the surface with light for deprotection</p> Signup and view all the answers

<p>Target presence, reversible reactions, and selective binding of active compounds</p> Signup and view all the answers

<p>Safety catch ensures the target molecule is safe on the linker until a specific step is performed</p> Signup and view all the answers

<p>By using different masks in each synthesis cycle</p> Signup and view all the answers

<p>PS allows for the generation of known structures at specific locations</p> Signup and view all the answers

<p>To test a vast number of compounds for biological activity.</p> Signup and view all the answers

<p>HTS assays are mostly optical assays, such as fluorescence, luminescence, and absorbance.</p> Signup and view all the answers

<p>The irreversible reaction used reduced all equilibrium products to stable compounds, shifting the equilibrium towards the active compound.</p> Signup and view all the answers

<p>The process involves freezing the equilibrium reactions and performing an irreversible reaction to convert all products to stable compounds.</p> Signup and view all the answers

<p>Irreversible reactions convert all equilibrium products to stable compounds, amplifying the active compound.</p> Signup and view all the answers

<p>HTS systems are heavily automated, using large compound storage facilities and computer-controlled robots for sample handling.</p> Signup and view all the answers