Structure Activity Relationships For Parasympathomimetic Drugs
For a cholinergic agent, the following criteria describe the structure activity relationship:
- 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.
- molecule must possess a nitrogen atom capable of bearing a positive charge, preferably a quaternary ammonium salt.
- for maximum potency, the size of the alkyl groups substituted on the nitrogen should not exceed the size of a methyl group.
- The molecule should have an oxygen atom, preferably an ester-like oxygen capable of participating in a hydrogen bond.
- There should be a two-carbon unit between the oxygen atom and the nitrogen atom.
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