SAR of Diphenyl Heptanone (Methadone Series)

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Chapter: Medicinal Chemistry : Narcotic Analgesics

The reduction of keto and acetylation of resulting hydroxyl group gives the acetyl methadol, the useful anti-diarrhoeal opioids, for example, diphenoxylate and loperamide.


SAR of Diphenyl Heptanone (Methadone Series)
  • The reduction of keto and acetylation of resulting hydroxyl group gives the acetyl methadol, the useful anti-diarrhoeal opioids, for example, diphenoxylate and loperamide.

  • Removal of any of the phenyl group sharply decreases the activity.

  • Placement of m-hydroxy group in the phenyl ring decreases analgesic activity.

  • The levo-isomer of methadone and isomethadone are twice as effective as their racemic mixture.

  • Substitution of terminal dimethylamino group by piperidine group decreases activity.

  • Substitution of propionyl group by hydrogen, hydroxyl or acetoxyl decreases the activity, whereas amide analogue, pyrrolidinoyl and terminal morpholino moiety enhance the activity by several time.

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