D.9.2 Explain the use of combinatorial and parallel chemistry to synthesize new drugs

Combinatorial Chemistry
  • Used to synthesize a large number of different compounds.
  • Produces an electronic database or combinatorial library.
  • The initial compound that demonstrates biological activity is called a lead compound, and is systematically modified to produce more effective derivatives.
  • Used to mass produce drugs by two solid-phase synthesis.

Solid-phase synthesis or mix and split:
  • starting material is covalently bonded to small polystyrene beads
  • beads are reacted with one another and then split and reacted with new substances to make new combination of molecules
  • produced a wide range of molecules
  • the products are then purified by filtering of the beads and washing
  • Used to build proteins (polypeptides)
  • This method is fully automated and uses robotics

Parallel synthesis
  • Used to produce smaller, more focused libraries