Parasympathomimetic Drug - Structure Activity Relationships For Parasympathomimetic Drugs

Structure Activity Relationships For Parasympathomimetic Drugs

For a cholinergic agent, the following criteria describe the structure activity relationship:

  1. Ing's Rule of 5: There should be no more than five atoms between the nitrogen and the terminal hydrogen for Muscarinic (or cholinergic) activity.
  2. molecule must possess a nitrogen atom capable of bearing a positive charge, preferably a quaternary ammonium salt.
  3. for maximum potency, the size of the alkyl groups substituted on the nitrogen should not exceed the size of a methyl group.
  4. The molecule should have an oxygen atom, preferably an ester-like oxygen capable of participating in a hydrogen bond.
  5. There should be a two-carbon unit between the oxygen atom and the nitrogen atom.

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