BPS 313 Lecture Notes - Lecture 40: Parent Structure, Partition Coefficient, Proteolysis
12 Sep 2016
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Document Summary
General techniques for preparing large libraries of compounds. Systemic + repetitive way by covalent assembly to give diverse array with common scaffold. Solid phase synthesis + automated synthetic machines. Mixtures of products formed in each rxn vessel. Products are physically distinct attached to different beads. Identities of structures in each vessel not known with certainty. Each mixture tested for activity as a mixture active mixtures are studied further to identify active component. Each experiment involves protection of amino acids, coupling and deprotection. Lecture 17: chapter 16 combinatorial + parallel synthesis . Deconvolution techniques needed to identify active compounds. Initial disappointment: the increase in molecules generated did not substantially change; # of compounds synthesized + screened increased. Reactants bound to polymeric surface, modified while still attached, final product released @ end of synthesis. Disadvantages: difficulty in scaling up reactions, alternative strategy is to carry out rxns in solution w. Number of possible different compounds in a library (n) excess reagent.
