SAR of Butyrophenones

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Chapter: Medicinal Chemistry : Tranquillizers

Antipsychotic activity is seen when Ar group is an aromatic system in which fluoro-substituents at para-position enhances the activity.


SAR of Butyrophenones


  • Antipsychotic activity is seen when Ar group is an aromatic system in which fluoro-substituents at para-position enhances the activity.

  • When X = carbonyl ( C = O) optimal activity is seen, although other groups C(H)OH, C(H) aryl (pimozide) also afford good activity.

  • When n = 3 activity is optimal, longer, or shorter chains decrease the activity.

  • Aliphatic amino nitrogen is required and highest activity is seen when it is incorporated into a cyclic form

  • Ar1 group should be an aromatic and is needed; it should be attached directly to the fourth position or occasionally separated from it by one intervening atom.

  • The Y group can vary and assist the activity.

  • The empirical SARs could be constructed to suggest that the 4-aryl piperidino moiety is super imposable on the 2-phenyl ethyl amino moiety of dopamine and accordingly could promote affinity for D2 and D3 receptors.

  • The long N-alkyl substituent could help to promote receptor affinity and produce receptor antagonism activity (or) inverse agonism.

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