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