SAR Solanaceous Alkaloids (Atropine Analogues)

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Chapter: Medicinal Chemistry : Anticholinergic Drugs

The greater molar potency of atropine helps to block several moles of acetylcholine.


SAR Solanaceous Alkaloids (Atropine Analogues)

Atropine


  • The greater molar potency of atropine helps to block several moles of acetylcholine.

  • The umbrella-like atropine molecule may mechanically or electrostatically inactivate adjacent receptors on the cell surface so that these receptors are also unavailable for acetylcholine or other parasympathomimetic stimulants.

  • The circled portion of the atropine molecule depicts the segment resembling acetylcholine.

  • The amine functional group is separated from the ester oxygen by more than two carbons, the conformation assumed by tropanol ring orients these two atoms such that the intervening distance is similar to that of acetylcholine. On the basis of the assumption that the size was a major factor in the blocking action, many substituted acetic acid ester of amino alcohol were prepared and evaluated for biological activity.

  • The most potent compounds were those that possessed two lipophilic ring substituents on the carbon alpha to carbonyl of ester moiety for antimuscarinic activity.

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